Elmisan 100 mg

INDICATIONS

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

PHARMACOLOGY

Pentosan polysulfate is a polymer of xylose hydrogen sulfate and contains two sulfate groups per carbohydrate monomer. It binds Fibroblast growth factors (FGFs) as well as other heparin-binding growth factors. It has been shown to interact also with the heparin-binding site of FGFR-1. It inhibits the growth of SW13 adrenocortical cells transfected with FGF-4 and tumorigenicity of MCF-7 breast carcinoma cells transfected with FGF-1 or FGF-4.

DOSAGE & ADMINISTRATION

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.

INTERACTION

In a study in which healthy subjects received pentosan polysulfate sodium 100 mg capsule or placebo every 8 hours for 7 days, and were titrated with warfarin to an INR of 1.4 to 1.8, the pharmacokinetic parameters of R-warfarin and S-warfarin were similar in the absence and presence of pentosan polysulfate sodium. INR for warfarin + placebo and warfarin + pentosan polysulfate sodium were comparable.

SIDE EFFECTS

Alopecia (4%), diarrhea (4%), nausea (4%), headache (3%), rash (3%), dyspepsia (2%), abdominal pain (2%), liver function abnormalities (1%), dizziness (1%).

PREGNANCY & LACTATION

Pregnancy: Reproduction studies have been performed in mice and rats with intravenous daily doses of 15 mg/kg, and in rabbits with 7.5 mg/kg. These doses are 0.42 and 0.14 times the daily oral human doses of Pentosan Polysulfate Sodium when normalized to body surface area. These studies did not reveal evidence of impaired fertility or harm to the fetus from Pentosan Polysulfate Sodium. Direct in vitro bathing of cultured mouse embryos with pentosan polysulfate sodium (PPS) at a concentration of 1 mg/mL may cause reversible limb bud abnormalities. Adequate and well-controlled studies have not been performed in pregnant women. Because animal studies are not always predictive of human response, this drug should be used in pregnancy only if clearly needed.Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Pentosan Polysulfate Sodium is administered to a nursing woman.

PRECAUTIONS & WARNINGS

Pentosan Polysulfate Sodium is a weak anticoagulant (1/15 the activity of heparin). At a daily dose of 300 mg (n=128), rectal hemorrhage was reported as an adverse event in 6.3% of patients. Bleeding complications of ecchymosis, epistaxis, and gum hemorrhage have been reported. Patients undergoing invasive procedures or having signs/symptoms of underlying coagulopathy or other increased risk of bleeding (due to other therapies such as coumarin anticoagulants, heparin, t-PA, streptokinase, high dose aspirin, or nonsteroidal anti inflammatory drugs) should be evaluated for hemorrhage. Patients with diseases such as aneurysms, thrombocytopenia, hemophilia, gastrointestinal ulcerations, polyps, or diverticula should be carefully evaluated before starting Pentosan Polysulfate Sodium. A similar product that was given subcutaneously, sublingually, or intramuscularly (and not initially metabolized by the liver) is associated with delayed immunoallergic thrombocytopenia with symptoms of thrombosis and hemorrhage. Caution should be exercised when using Pentosan Polysulfate Sodium in patients who have a history of heparin induced thrombocytopenia. Alopecia is associated with pentosan polysulfate and with heparin products. In clinical trials of Pentosan Polysulfate Sodium, alopecia began within the first 4 weeks of treatment. Ninety-seven percent (97%) of the cases of alopecia reported were alopecia areata, limited to a single area on the scalp.

THERAPEUTIC CLASS

Other genito-urinary preparations

STORAGE CONDITIONS

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.