Pentosan polysulfate sodium is indicated for the relief of bladder pain and discomfort associated with interstitial cystitis.

Pentosan polysulfate is a semi-synthetic polysaccharide composed of xylose hydrogen sulfate units, containing two sulfate groups per carbohydrate monomer. It binds to fibroblast growth factors (FGFs) and other heparin-binding growth factors. It also interacts with the heparin-binding site of FGFR-1 (fibroblast growth factor receptor-1). It inhibits the growth of SW13 adrenocortical cells transfected with FGF-4 and reduces the tumorigenicity of MCF-7 breast carcinoma cells transfected with FGF-1 or FGF-4.

The recommended dose of Pentosan Polysulfate Sodium is 300 mg/day taken as one 100 mg capsule orally three times daily. The capsules should be taken with water at least 1 hour before meals or 2 hours after meals. Patients receiving Pentosan Polysulfate Sodium should be reassessed after 3 months. If improvement has not occurred and if limiting adverse events are not present, Pentosan Polysulfate Sodium may be continued for another 3 months. The clinical value and risks of continued treatment in patients whose pain has not improved by 6 months is not known.

Pediatric Use: Safety and effectiveness in pediatric patients below the age of 16 years have not been established

In a clinical study, healthy subjects received Pentosan Polysulfate Sodium 100 mg every 8 hours for 7 days along with warfarin titrated to an INR of 1.4–1.8. The pharmacokinetic parameters of R-warfarin and S-warfarin were similar whether pentosan polysulfate sodium was present or not. INR values were also comparable between warfarin alone and warfarin with pentosan polysulfate sodium.

Pentosan Polysulfate Sodium is contraindicated in patients with known hypersensitivity to the drug, related compounds, or any excipients in the formulation.

Common adverse effects include: Alopecia (4%), Diarrhea (4%) ,Nausea (4%), Headache (3%), Rash (3%), Dyspepsia (2%), Abdominal pain (2%), Liver function abnormalities (1%), Dizziness (1%).

Pregnancy: Reproductive studies in animals (mice, rats, and rabbits) at doses up to 0.42 and 0.14 times the human dose did not show impaired fertility or fetal harm. However, in vitro studies showed that high concentrations may cause reversible limb bud abnormalities in mouse embryos. Adequate controlled studies in pregnant women are lacking. Therefore, use during pregnancy only if clearly needed.

Lactation: It is not known whether the drug is excreted in human milk. Since many drugs pass into breast milk, caution is advised when administering to nursing mothers.

Pentosan Polysulfate Sodium has weak anticoagulant activity (about 1/15 that of heparin). At a dose of 300 mg/day, rectal bleeding has been reported in 6.3% of patients. Other bleeding events include bruising, nosebleeds, and gum bleeding. Patients at risk of bleeding or on anticoagulants, antiplatelets, thrombolytics, or NSAIDs should be carefully evaluated. Caution is required in patients with aneurysms, thrombocytopenia, hemophilia, gastrointestinal ulcers, polyps, or diverticula. Rare cases of immune-mediated thrombocytopenia have been reported with related heparin-like compounds. Alopecia may occur, usually within the first 4 weeks, most commonly as localized alopecia areata.

Other genito-urinary preparations

Store below 30°C in a cool, dry place, away from light and moisture. Keep out of reach of children.