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Pentosan Polysulfate Sodium


General


Pronunciation

(PEN toe san pol i SUL fate SOW dee um)


Brand Names: U.S.

  • Elmiron

Indications


Use: Labeled Indications

Relief of bladder pain or discomfort due to interstitial cystitis


Contraindications


Hypersensitivity to pentosan polysulfate sodium, related compounds (LMWHs or heparin), or any component of the formulation


Dosing and Administration


Dosing: Adult

Interstitial cystitis: Oral: 100 mg 3 times/day taken with water 1 hour before or 2 hours after meals

Note: Patients should be evaluated at 3 months and may be continued an additional 3 months if there has been no improvement and if there are no therapy-limiting side effects. The risks and benefits of continued use beyond 6 months in patients who have not responded is not yet known.


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Children ≥16 years: Refer to adult dosing.


Dosing: Renal Impairment

No dosage adjustment provided in manufacturer 's labeling (has not been studied).


Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer 's labeling (has not been studied). However, dosage adjustment may be necessary due to hepatic impairment impact on pharmacokinetics. Use with caution.


Administration

Should be administered with water 1 hour before or 2 hours after meals.


Dietary Considerations

Should be taken with water 1 hour before or 2 hours after meals.


Storage

Store at room temperature of 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Elmiron: 100 mg [contains fd&c blue #1 aluminum lake, fd&c blue #2 aluminum lake, fd&c red #40 aluminum lake, fd&c yellow #10 aluminum lake]


Drug Interactions

Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): Pentosan Polysulfate Sodium may enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Specifically, the risk of bleeding may be increased by concurrent use of these agents. Monitor therapy

Anticoagulants: Pentosan Polysulfate Sodium may enhance the anticoagulant effect of Anticoagulants. Monitor therapy


Adverse Reactions


1% to 10%:

Central nervous system: Headache (3%), dizziness (1%)

Dermatologic: Alopecia (4%), rash (3%)

Gastrointestinal: Rectal hemorrhage (6%), diarrhea (4%), nausea (4%), abdominal pain (2%), dyspepsia (2%)

Hepatic: Liver function test abnormalities (1%; dose related)

<1% (Limited to important or life-threatening): Allergic reactions, amblyopia, anemia, anorexia, colitis, conjunctivitis, constipation, dehydration, depression, diaphoresis, dyspnea, ecchymosis, emotional lability, epistaxis, esophagitis, flatulence, gastritis, gum bleeding, hyperkinesia, increased partial thromboplastin time, insomnia, leukopenia, mouth ulcer, optic neuritis, pharyngitis, photosensitivity, pruritus, PT prolonged, retinal hemorrhage, rhinitis, thrombocytopenia, tinnitus, urticaria, vomiting


Warnings/Precautions


Concerns related to adverse effects:

- Bleeding: Pentosan polysulfate is a low-molecular weight heparin-like compound with anticoagulant and fibrinolytic effects, therefore, bleeding complications (such as ecchymosis, epistaxis, and gum bleeding) may occur. Patients undergoing invasive procedures or having signs or symptoms of underlying coagulopathies or other increased risk of bleeding (eg, receiving heparin, warfarin, thrombolytics, NSAIDs, or high dose aspirin) should be evaluated prior to use.

Disease-related concerns:

- Aneurysm: Carefully evaluate patients with aneurysm before initiating therapy.

- Bleeding disorders: Carefully evaluate patients with hemophilia and/or thrombocytopenia before initiating therapy.

- Gastrointestinal disease: Carefully evaluate patients with gastrointestinal ulcerations, polyps, and/or diverticula before initiating therapy.

- Heparin-induced thrombocytopenia: Use with caution in patients with a history of heparin-induced thrombocytopenia.

- Hepatic impairment: Use with caution in patients with hepatic impairment.

Special populations:

- Pediatric: Safety and efficacy have not been established in children <16 years of age.


Pregnancy Risk Factor

B


Pregnancy Considerations

No adverse events were noted in animal reproduction studies; however, reversible limb bud abnormalities were noted during in vitro animal studies. There are no adequate and well-controlled studies in pregnant women. Use with caution and only if clearly needed during pregnancy. Based on limited data, pentosan polysulfate does not appear to cross the placenta.


Actions


Pharmacology

Although pentosan polysulfate sodium is a low-molecular weight heparinoid, it is not known whether these properties play a role in its mechanism of action in treating interstitial cystitis; the drug appears to adhere to the bladder wall mucosa where it may act as a buffer to protect the tissues from irritating substances in the urine.


Absorption

~6%


Metabolism

Hepatic and splenic via partial desulfation; partial depolymerization occurs in the renal parenchyma; saturable


Excretion

Feces (58% to 84%, as unchanged drug); urine (6%, primarily as metabolites)


Time to Peak

Serum: 2 hours (range: 0.6-120 hours)


Half-Life Elimination

20-27 hours


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience nausea, vomiting, diarrhea, headache, or hair loss. Have patient report immediately to prescriber bruising; bleeding; nose bleeds; severe loss of strength and energy; bleeding in eye; or black, tarry, or bloody stools (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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