pinaverium

Action and Spectrum

Actions and Spectrum: 

pinaverium is a medication used primarily to treat functional gastrointestinal disorders, like irritable bowel syndrome. It acts as a spasmolytic agent, meaning it helps to relax and reduce muscle spasms in the gastrointestinal tract. This, in turn, can alleviate symptoms like abdominal pain, bloating, and changes in bowel habits. 

Action: 

• Smooth muscle relaxation: pinaverium exerts its pharmacological action by selectively blocking the L-type calcium channels in the smooth muscle cells of the GIT (gastrointestinal tract). These channels allow calcium ions to enter the muscle cells, leading to muscle contraction. By blocking these channels, pinaverium inhibits the influx of calcium, resulting in the relaxation of the smooth muscles in the gut. 
• Decreased gut motility: By relaxing the smooth muscles, pinaverium reduces the motility of the gastrointestinal tract. This reduction in gut motility can be beneficial in conditions where excessive or uncoordinated muscle contractions are causing discomfort and symptoms. 

Spectrum:  

The spectrum of pinaverium’s action is primarily limited to the gastrointestinal tract. It acts locally within the gut to alleviate symptoms associated with functional gastrointestinal disorders. pinaverium is not absorbed significantly into the bloodstream, which means it has minimal systemic effects. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Heartburn 

Nausea 

Abdominal pain 

Headache 

Constipation 

Dry mouth 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity to pinaverium: Individuals with known hypersensitivity or allergy to pinaverium or its components should not use this medication. 
• Severe Liver Dysfunction: pinaverium is primarily metabolized in the liver, so individuals with severe liver impairment should avoid its use. The medication’s safety and effectiveness in such cases have not been established. 
• Children: pinaverium is generally not recommended for children, as its safety and efficacy in pediatric populations have not been well-studied. 
• Pregnancy and Breastfeeding: The safety of pinaverium during pregnancy and breastfeeding has not been conclusively established. Therefore, it is generally avoided during these periods unless the potential benefits outweigh the risks and only under the supervision of a healthcare professional. 
• Bowel Obstruction: pinaverium is not suitable for individuals with mechanical bowel obstruction since its smooth muscle relaxing action may exacerbate the condition. 
• Inflammatory Bowel Diseases: Individuals with active inflammatory bowel diseases (such as Crohn’s disease or ulcerative colitis) may need to avoid pinaverium, as it may not be effective in treating these conditions and might worsen symptoms. 
• Intestinal Perforation: pinaverium should not be used in patients with a history of intestinal perforation, as it may mask symptoms or delay diagnosis. 

Caution 

• Elderly Patients: Caution should be exercised when prescribing pinaverium to elderly individuals, as they may be more susceptible to specific side effects or drug interactions. Dosing adjustments or close monitoring may be necessary. 
• Mild to Moderate Liver Dysfunction: pinaverium is primarily metabolized in the liver. Therefore, caution should be exercised when using pinaverium in patients with mild-moderate liver impairment.  
• Interaction with Other Medications: Before starting pinaverium, inform your healthcare provider about all the drugs you are taking, including prescription and OTC (over-the-counter) drugs, as well as herbal supplements. Some medications may interact with pinaverium, affecting its effectiveness/increasing the risk of side effects. 
• Gastrointestinal Disorders: While pinaverium treats functional gastrointestinal disorders like irritable bowel syndrome (IBS), caution is advised if you have other underlying gastrointestinal conditions. Your doctor must evaluate your case and determine if pinaverium suits you. 
• Pregnancy and Breastfeeding: As mentioned earlier, the safety of pinaverium during pregnancy and breastfeeding is not well-established.  
• Allergic Reactions: If you experience any signs of an allergic reaction, like itching, swelling, rash, dizziness, or difficulty breathing, stop using pinaverium immediately and seek medical attention. 
• Driving and Operating Machinery: pinaverium is not known to cause drowsiness or impair cognitive function. However, individual responses to medications may vary. If you experience dizziness or other side effects affecting your ability to drive/operate machinery safely, avoid such activities until you know how the medication affects you. 
• Discontinuation: Do not stop or change the dosage of pinaverium without consulting your healthcare provider, even if you feel better. Abruptly stopping the medication may lead to a recurrence of symptoms. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

pinaverium is a spasmolytic agent with a selective action on the gastrointestinal tract. It exerts its pharmacological effects by blocking L-type calcium channels in smooth muscle cells. By inhibiting the influx of calcium ions, pinaverium induces smooth muscle relaxation, reducing gut motility and alleviating symptoms in functional gastrointestinal disorders, such as irritable bowel syndrome (IBS).

Its local action within the gastrointestinal tract minimizes systemic effects, contributing to its favorable safety profile. As a result, pinaverium is widely used to manage symptoms associated with functional gastrointestinal disorders, relieving abdominal pain, cramping, bloating, and irregular bowel habits. 

Pharmacodynamics: 

Mechanism of action: The action of pinaverium involves its specific effect on the smooth muscle cells in the gastrointestinal (GI) tract. It is considered a calcium channel blocker with selectivity for the L-type calcium channels in smooth muscle cells.  

pinaverium acts by binding to these L-type calcium channels, thus inhibiting the influx of calcium ions into the smooth muscle cells of the GI tract. As a result, the contractile response of the smooth muscles is reduced, leading to relaxation. This smooth muscle relaxation helps to relieve spasms and hypermotility in the GI tract. 

By reducing excessive muscle contractions and calming the smooth muscles of the gastrointestinal tract, pinaverium effectively alleviates symptoms associated with functional gastrointestinal disorders, such as irritable bowel syndrome (IBS). These symptoms may include abdominal pain, cramping, bloating, and irregular bowel movements. 

Pharmacokinetics: 

Absorption 

pinaverium is administered orally in the form of tablets. After ingestion, it is absorbed from the gastrointestinal tract into the bloodstream. 

Distribution 

Once absorbed, pinaverium is likely to distribute throughout the body. However, its distribution is expected to be confined mainly to the gastrointestinal tissues, where it exerts its pharmacological effects. 

Metabolism 

pinaverium undergoes hepatic metabolism, primarily in the liver. More details about the enzymes involved in its metabolism are widely available. Nevertheless, the metabolism of pinaverium might involve biotransformation processes that convert the drug into metabolites for subsequent elimination. 

Elimination and Excretion 

The elimination of pinaverium and its metabolites is mainly through feces (biliary excretion) rather than urine. This suggests that pinaverium and its metabolites are likely excreted through the hepatobiliary route, with minimal renal excretion. 

Adminstartion

Administration: 

Oral administration 

• Dosage: The dosage of pinaverium may vary depending on the specific product and the condition being treated. Always follow the prescribed dosage and instructions provided by your healthcare professional. 
• Timing: pinaverium is usually taken before meals. Taking the tablet about 15-30 minutes before a meal is recommended to allow sufficient time for the medication to start working before the food is consumed. 
• Swallowing: Swallow the tablet whole with a glass of water. Do not chew, crush/break the tablet, which may affect its efficacy. 
• Food Interactions: While pinaverium is generally taken before meals, it is still essential to follow any specific instructions your healthcare provider gives regarding food interactions, if any. 
• Duration of Treatment: Your healthcare provider will determine the duration of treatment with pinaverium based on the nature and severity of your condition. Follow the prescribed course of treatment even if your symptoms improve unless instructed otherwise by your doctor. 
• Missed Dose: If you miss a dose, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for the missed one. 
• Overdose: In case of accidental overdose, seek immediate medical attention or contact your local poison control center. 
• Storage: Store pinaverium tablets at room temperature, away from moisture and heat. Keep the medication out of the reach of children. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: pinaverium 

Why do we use pinaverium? 

pinaverium is a medication primarily used to treat functional gastrointestinal disorders, incredibly irritable bowel syndrome (IBS).  

• Irritable Bowel Syndrome (IBS): pinaverium is commonly prescribed to manage the symptoms of IBS (irritable bowel syndrome). IBS is a chronic gastrointestinal disorder which is characterized by abdominal pain, bloating, and changes in bowel habits, like diarrhea, constipation, or alternating between the two. pinaverium helps to relieve these symptoms by reducing smooth muscle spasms in the gastrointestinal tract. 
• Functional Gastrointestinal Disorders: Besides IBS, pinaverium may also treat other functional gastrointestinal disorders characterized by symptoms like abdominal discomfort, pain, and irregular bowel movements.