Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Pinaverium is a Calcium Channel Blocker belonging to Gastrointestinal agent.
Pinaverium is a spasmolytic agent used for the symptomatic treatment of irritable bowel syndrome (IBS) and functional disorders of the biliary tract.
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. Pinaverium is highly bound to human plasma proteins with the ratio of 97%. 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. Pinaverium is predominantly eliminated into feces. The mean elimination half-life is approximately 1.5 hours.
Pinaverium shows side effects like Chest pain, Cough, Headache, Dizziness, Stomach pain, Diarrhea, Nausea, Vomiting, Dry mouth, Skin Rash, Difficulty in swallowing.
Pinaverium is available in the form of Oral Tablet.
Pinaverium is available in India, Canada, South Korea, UK, Indonesia, Singapore, Malaysia, and Australia.
Pinaverium belongs to the Gastrointestinal agent acts as a Calcium Channel Blocker.
Pinaverium interacts with the 1,4-dihydropyridine binding sites on voltage dependent L-type calcium channels located on GI smooth muscle cells in a competitive manner. The binding site is in the alpha 1S subunit and pinaverium most likely antagonizes the action of calcium ions by stabilizing a non-conducting channel state. Pinaverium 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.
The Data of Onset and duration of action of Pinaverium is not clinically established.
The Tmax of Pinaverium is approximately 1 hour.
Pinaverium is available in the form of Oral Tablet.
Pinaverium tablet is taken orally, usually three times a day.
Pinaverium is used to treat and relieve the symptoms such as abdominal pain and cramps associated with irritable bowel syndrome. It is also used to treat the functional disorders of the biliary tract as well as in preparation for a barium enema.
Pinaverium is a Calcium Channel Blocker belonging to Gastrointestinal agent.
Pinaverium is approved for use in the following clinical indications
- Biliary disorders, irritable bowel syndrome
Pinaverium is a spasmolytic agent used for the symptomatic treatment of irritable bowel syndrome (IBS) and functional disorders of the biliary tract.
- Biliary disorders, irritable bowel syndrome
Oral: Initial: 50 mg 3 times/day; dose may be increased up to 100 mg 3 times/day (maximum dose: 300 mg/day).
Pinaverium is available in various strengths as 50mg and 100mg.
Pinaverium is available in the form of Oral tablet.
Pinaverium is contraindicated in patients with
- Hypersensitivity to pinaverium or any component of the formulation.
- Esophageal irritation
May cause esophageal irritation; minimize risk by administering with a full glass of water with a meal/snack (do not crush/chew or suck tablets). Patients must be advised not to take medication when lying down or at bedtime. Use caution in patients with possible gastroesophageal reflux or hiatal hernia.
- GI motility
Avoid using to treat motility dysfunction associated with underlying disease states.
- Hereditary galactose intolerance
Contains lactose; avoid use in patients with hereditary problems of galactose intolerance, congenital lactase deficiency, or glucose-galactose malabsorption.
Breast Feeding Warning
Pinaverium is not recommended for use in breastfeeding women unless necessary. All the risks and benefits should be taken into consideration before taking this medicine.
Pregnancy Warning
Pinaverium is not recommended for use in pregnant women unless necessary. All the risks and benefits should be taken into consideration before taking this medicine.
Common
- Allergic skin reaction, Abdominal distention, constipation, diarrhea, epigastric fullness, epigastric pain, heartburn, nausea, xerostomia, Drowsiness, headache, vertigo.
Rare
- Rash, Erythema of skin, pruritus, skin rash, urticaria, Abdominal pain, dysphagia, vomiting, Anaphylactic shock, angioedema, hypersensitivity reaction.
The common side effects of Pinaverium include the following
- Common side effects
Chest pain, Cough, Headache, Dizziness, Stomach pain, Diarrhea, Nausea, Vomiting, Dry mouth, Skin Rash, Difficulty in swallowing.
- Pregnancy
Pregnancy Category
Pinaverium is not recommended for use in pregnant women unless necessary. All the risks and benefits should be taken into consideration before taking this medicine.
- Nursing Mothers
Pinaverium is not recommended for use in breastfeeding women unless necessary. All the risks and benefits should be taken into consideration before taking this medicine.
- Pediatric Use
This medicine is not recommended for use in children below 18 years of age since the safety and efficacy of use are not clinically established.
Pharmacodynamic
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. At higher concentrations, pinaverium also exhibits very weak anticholinergic effects but is not shown to display vasodilatory or anti-arrhythmic actions.
Pharmacokinetics
- Absorption
After oral administration, pinaverium is poorly absorbed (5-10%) followed by uptake by liver. Peak plasma concentration is reached within one hour after administration
- Distribution
Pinaverium is highly bound to human plasma proteins with the ratio of 97%.
- Metabolism and Excretion
Pinaverium is extensively metabolized via Hepatic route via demethylation, hydroxylation. Pinaverium is predominantly eliminated into feces.
- Zheng L, Lai Y, Lu W, Li B, Fan H, Yan Z, Gong C, Wan X, Wu J, Huang D, Wang Y. Pinaverium reduces symptoms of irritable bowel syndrome in a multicenter, randomized, controlled trial. Clinical Gastroenterology and Hepatology. 2015 Jul 1;13(7):1285-92.
- Sheng C, Dongqing D, Yuxia M, Qi X, Shuzhong G, Xiuying W. Clinical study on herbal cone-partitioned moxibustion for irritable bowel syndrome due to spleen-qi deficiency. Journal of Acupuncture and Tuina Science. 2011;5(9):265-8.
- Christen MM, Tassignon JP. Pinaverium bromide: A calcium channel blocker acting selectively on the gastrointestinal tract. Drug development research. 1989;18(2):101-12.
- https://www.uptodate.com/contents/pinaverium-united-states-not-available-drug-information?search=pinaverium&source=panel_search_result&selectedTitle=1~3&usage_type=panel&kp_tab=drug_general&display_rank=1
- https://www.practo.com/medicine-info/pinaverium-bromide-2173-api#:~:text=Description,preparation for a barium enema.
- https://go.drugbank.com/drugs/DB09090
