pentosan polysulfate sodium

Action and Spectrum

Actions and Spectrum: 

• The mechanism of action of pentosan polysulfate sodium has yet to be fully understood, but it is thought to have several different effects on the body. 
• One of the primary actions of pentosan polysulfate sodium is its ability to protect the bladder lining. It does this by increasing the production of glycosaminoglycans (GAGs), natural substances that help protect and lubricate the bladder wall. By increasing GAG production, pentosan polysulfate sodium helps to improve the integrity of the bladder lining and reduce inflammation. 
• pentosan polysulfate sodium is also believed to have anti-inflammatory properties. It has been shown to inhibit the production of pro-inflammatory cytokines, which are molecules that contribute to inflammation and pain. This anti-inflammatory effect is thought to help reduce the symptoms of IC and other inflammatory conditions. 
• Regarding its spectrum of activity, pentosan polysulfate sodium is primarily used to treat interstitial cystitis. Still, it has also been used to treat other conditions, such as osteoarthritis and deep vein thrombosis. 

Drug Interaction

Adverse Reaction

Frequency not defined 

1-10% 

Diarrhea (4%) 

Headache (3%) 

Indigestion (2%) 

Alopecia (4%) 

Nausea (4%) 

Abdominal pain (2%) 

Post-marketing reports 

Elevated LFTs 

Leukopenia 

Prothrombin time increased 

Optic neuritis 

Pigmentary changes in the retina 

Rectal hemorrhage 

Anemia 

Partial thromboplastin time increased 

Thrombocytopenia 

Retinal hemorrhage 

Black Box Warning

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity or allergy to the medication or its components. 
• Bleeding disorders: pentosan polysulfate sodium can increase the risk of bleeding, so it should not be used in individuals with bleeding disorders, such as hemophilia. 
• Pregnancy and breastfeeding: The safety of pentosan polysulfate sodium in pregnant or breastfeeding women is not well established, so it should be avoided unless the benefits outweigh the potential risks. 
• Renal impairment: pentosan polysulfate sodium is cleared from the body through the kidneys. Individuals with significant renal impairment may experience increased levels of the drug in their system, which can increase the risk of side effects. 
• Recent surgery: pentosan polysulfate sodium should not be used in individuals who have had recent surgery or a procedure that may cause bleeding, such as dental work or a biopsy. 
• Liver impairment: pentosan polysulfate sodium should be used cautiously in individuals with liver impairment, as it can increase the risk of bleeding. 
• Use with anticoagulants: pentosan polysulfate sodium can increase the risk of bleeding when used with anticoagulant medications, such as warfarin or heparin. Therefore, caution should be exercised when using it with these medications. 

Caution: 

• Drug interactions: pentosan polysulfate sodium can interact with certain medications, such as blood thinners, and increase the risk of bleeding. Therefore, caution should be exercised when using it with these medications. 
• Renal function: pentosan polysulfate sodium is primarily cleared from the body through the kidneys, so individuals with renal impairment may experience increased levels of the drug in their system, which can increase the risk of side effects. 
• Bleeding disorders: pentosan polysulfate sodium can increase the risk of bleeding, so caution should be exercised in individuals with bleeding disorders. 
• Surgery: pentosan polysulfate sodium should be discontinued before elective surgery or procedures that may cause bleeding. 
• Skin reactions: pentosan polysulfate sodium has been associated with skin reactions, such as rash or itching, so caution should be exercised in individuals with a history of skin allergies. 
• Monitoring: Regular monitoring of renal function and blood coagulation parameters may be necessary for individuals taking pentosan polysulfate sodium  
• Pediatric use: The safety and efficacy of pentosan polysulfate sodium in children have not been well established, so caution should be exercised when using pentosan polysulfate sodium in pediatric patients. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: B 

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: 

• pentosan polysulfate sodium (PPS) is a semi-synthetic polysaccharide derivative with anti-inflammatory, anticoagulant, and cytoprotective properties. PPS comprises chains of xylose and sulfated glucuronic acid and has a high negative charge density, contributing to its ability to interact with various proteins and cells in the body. 
• PPS is thought to work by increasing the production of glycosaminoglycans (GAGs), natural substances found in the bladder lining and other tissues throughout the body. GAGs are essential for maintaining the integrity of the bladder wall and reducing inflammation. By increasing GAG production, PPS helps to improve the bladder lining and reduce inflammation. 
• PPS also has anticoagulant properties, which can help to prevent blood clots. It works by binding to antithrombin III, a natural protein in the blood that inhibits blood clotting. By binding to antithrombin III, PPS increases its activity and prolongs the time it takes for blood to clot. 
• In addition, PPS has been shown to have antioxidant and cytoprotective effects, which can help to protect cells and tissues from damage caused by oxidative stress and inflammation. 

Pharmacodynamics: 

The pharmacodynamics of pentosan polysulfate sodium (PPS) involves its interactions with various body components, including the bladder lining, blood, and cells. 

• PPS is known to increase the production of glycosaminoglycans (GAGs), natural substances found in the bladder lining and other tissues throughout the body. GAGs are essential for maintaining the integrity of the bladder wall and reducing inflammation. By increasing GAG production, PPS helps to improve the bladder lining and reduce inflammation. PPS has also been shown to increase the production of hyaluronic acid, another natural substance that helps protect the bladder lining. 
• PPS has anticoagulant properties due to its ability to bind to antithrombin III, a natural protein in the blood that inhibits blood clotting. By binding to antithrombin III, PPS increases its activity and prolongs the time it takes for blood to clot. This effect can help prevent blood clots, but it can also increase the risk of bleeding. 
• PPS has been shown to have antioxidant and cytoprotective effects, which can help protect cells and tissues from damage caused by oxidative stress and inflammation damage. PPS has been shown to scavenge free radicals and reduce the production of reactive oxygen species, which can damage cells and tissues. 

Pharmacokinetics: 

Absorption 

It is rapidly absorbed after oral administration, with peak plasma concentrations reached within 2 to 4 hours. pentosan polysulfate sodium absorption depends on the dose, with higher doses leading to greater plasma concentrations. 

Distribution 

pentosan polysulfate sodium is widely distributed throughout the body, with the highest concentrations in the liver, kidneys, and bladder. It is highly bound to plasma proteins, which limits its distribution to tissues. 

Metabolism 

pentosan polysulfate sodium is primarily excreted unchanged in the urine, with minimal metabolism in the liver. However, some studies suggest that it may undergo limited metabolism in the gastrointestinal tract, where it is hydrolyzed to lower molecular weight fragments. 

Elimination and Excretion 

pentosan polysulfate sodium is primarily excreted in the urine, with a half-life of approximately 4 to 6 hours. The renal clearance of pentosan polysulfate sodium is dose-dependent, with higher doses leading to greater renal excretion. 

Adminstartion

Administration: 

The dosage and administration of pentosan polysulfate sodium may vary depending on the individual’s age, medical condition, and response to treatment. It is essential to follow the instructions provided by your healthcare provider. 

Typically, the initial dosage of pentosan polysulfate sodium is 100 mg injected into a muscle or under the skin once weekly for six weeks, followed by a maintenance dosage of 100 mg every 2 to 4 weeks. Your healthcare provider may adjust the dosage and frequency of administration based on your response to treatment. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: pentosan polysulfate sodium 

Why do we use pentosan polysulfate sodium? 

pentosan polysulfate sodium is a medication used primarily for treating bladder pain syndrome, also known as interstitial cystitis. This condition is characterized by chronic pain, discomfort in the bladder and pelvic region, and frequent urination. 

pentosan polysulfate sodium is thought to work by restoring the bladder’s protective lining and reducing inflammation in the bladder tissues. This can help to alleviate symptoms such as pain, urgency, and frequency of urination. 

In addition to its use for bladder pain syndrome, pentosan polysulfate sodium has also been studied for its potential benefits in other conditions, such as osteoarthritis and deep vein thrombosis.