Elmiron
(pentosan polysulfate)By using PrescriberAI, you agree to the AI Terms of Use.
Elmiron Prescribing Information
ELMIRON ®(pentosan polysulfate sodium) is indicated for the relief of bladder pain or discomfort associated with interstitial cystitis.
The recommended dose of ELMIRON ®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 ELMIRON ®should be reassessed after 3 months. If improvement has not occurred and if limiting adverse events are not present, ELMIRON ®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.
ELMIRON ®is contraindicated in patients with known hypersensitivity to the drug, structurally related compounds, or excipients.
ELMIRON ®was evaluated in clinical trials in a total of 2627 patients (2343 women, 262 men, 22 unknown) with a mean age of 47 [range 18 to 88 with 581 (22%) over 60 years of age]. Of the 2627 patients, 128 patients were in a 3-month trial and the remaining 2499 patients were in a long-term, unblinded trial.
Deaths occurred in 6/2627 (0.2%) patients who received the drug over a period of 3 to 75 months. The deaths appear to be related to other concurrent illnesses or procedures, except in one patient for whom the cause was not known.
Serious adverse events occurred in 33/2627 (1.3%) patients. Two patients had severe abdominal pain or diarrhea and dehydration that required hospitalization. Because there was not a control group of patients with interstitial cystitis who were concurrently evaluated, it is difficult to determine which events are associated with ELMIRON ®and which events are associated with concurrent illness, medicine, or other factors.
| Body System/Adverse Experience | ELMIRON ® n=128 | Placebo n=130 |
|---|---|---|
| ||
| CNSOverall Number of Patients * | 3 | 5 |
| Insomnia | 1 | 0 |
| Headache | 1 | 3 |
| Severe Emotional Lability/Depression | 2 | 1 |
| Nystagmus/Dizziness | 1 | 1 |
| Hyperkinesia | 1 | 1 |
| GIOverall Number of Patients * | 7 | 7 |
| Nausea | 3 | 3 |
| Diarrhea | 3 | 6 |
| Dyspepsia | 1 | 0 |
| Jaundice | 0 | 1 |
| Vomiting | 0 | 2 |
| Skin/AllergicOverall Number of Patients * | 2 | 4 |
| Rash | 0 | 2 |
| Pruritus | 0 | 2 |
| Lacrimation | 1 | 1 |
| Rhinitis | 1 | 1 |
| Increased Sweating | 1 | 0 |
| OtherOverall Number of Patients * | 1 | 3 |
| Amenorrhea | 0 | 1 |
| Arthralgia | 0 | 1 |
| Vaginitis | 1 | 1 |
| Total Events | 17 | 27 |
| Total Number of Patients Reporting Adverse Events | 13 | 19 |
The adverse events described below were reported in an unblinded clinical trial of 2499 interstitial cystitis patients treated with ELMIRON ®. Of the original 2499 patients, 1192 (48%) received ELMIRON ®for 3 months; 892 (36%) received ELMIRON ®for 6 months; and 598 (24%) received ELMIRON ®for one year, 355 (14%) received ELMIRON ®for 2 years, and 145 (6%) for 4 years.
Frequency (1 to 4%): Alopecia (4%), diarrhea (4%), nausea (4%), headache (3%), rash (3%), dyspepsia (2%), abdominal pain (2%), liver function abnormalities (1%), dizziness (1%).
Frequency (≤ 1%):
Digestive:Vomiting, mouth ulcer, colitis, esophagitis, gastritis, flatulence, constipation, anorexia, gum hemorrhage.
Hematologic:Anemia, ecchymosis, increased prothrombin time, increased partial thromboplastin time, leukopenia, thrombocytopenia.
Hypersensitive Reactions:Allergic reaction, photosensitivity.
Respiratory System:Pharyngitis, rhinitis, epistaxis, dyspnea.
Skin and Appendages:Pruritus, urticaria.
Special Senses:Conjunctivitis, tinnitus, optic neuritis, amblyopia, retinal hemorrhage.
Post-Marketing Experience
The following adverse reactions have been identified during post approval use of pentosan polysulfate sodium; because these reactions were reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure:
- pigmentary changes in the retina (see WARNINGS).
Rectal Hemorrhage
ELMIRON ®was evaluated in a randomized, double-blind, parallel group, Phase 4 study conducted in 380 patients with interstitial cystitis dosed for 32 weeks. At a daily dose of 300 mg (n=128), rectal hemorrhage was reported as an adverse event in 6.3% of patients. The severity of the events was described as "mild" in most patients. Patients in that study who were administered ELMIRON ®900 mg daily, a dose higher than the approved dose, experienced a higher incidence of rectal hemorrhage, 15%.
Liver Function Abnormality
A randomized, double-blind, parallel group, Phase 2 study was conducted in 100 men (51 ELMIRON ®and 49 placebo) dosed for 16 weeks. At a daily dose of 900 mg, a dose higher than the approved dose, elevated liver function tests were reported as an adverse event in 11.8% (n=6) of ELMIRON ®-treated patients and 2% (n=1) of placebo-treated patients.
Drug-Drug Interactions
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. See also PRECAUTIONSon the use of ELMIRON ®in patients receiving other therapies with anticoagulant effects.
Pentosan polysulfate sodium is a semi-synthetically produced heparin-like macromolecular carbohydrate derivative, which chemically and structurally resembles glycosaminoglycans. It is a white odorless powder, slightly hygroscopic and soluble in water to 50% at pH 6. It has a molecular weight of 4000 to 6000 Dalton with the following structural formula:
ELMIRON ®is supplied in white, opaque hard gelatin capsules containing 100 mg pentosan polysulfate sodium, microcrystalline cellulose, and magnesium stearate. It also contains pharmaceutical glaze (modified) in SD-45, synthetic black iron oxide, FD&C Blue No. 2 aluminum lake, FD&C Red No. 40 aluminum lake, FD&C Blue No. 1 aluminum lake, D&C Yellow No. 10 aluminum lake, n-butyl alcohol, propylene glycol, SDA-3A alcohol, and titanium dioxide. It is formulated for oral use.