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Pentosan Polysulfate Sodium

Medically reviewed by Drugs.com. Last updated on Sep 11, 2020.

Pronunciation

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

Index Terms

  • PPS

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]

Brand Names: U.S.

  • Elmiron

Pharmacologic Category

  • Analgesic, Urinary

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

Use: Labeled Indications

Interstitial cystitis: Relief of bladder pain or discomfort due to interstitial cystitis

Contraindications

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

Dosing: Adult

Interstitial cystitis: Oral: 100 mg 3 times daily

Note: Patients should be re-evaluated after 3 months; therapy may continue for 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

Interstitial cystitis: Adolescents ≥16 years: Oral: Refer to adult dosing.

Administration

Administer 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).

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%:

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

Endocrine & metabolic: Increased gamma-glutamyl transferase (1%, transient), increased lactate dehydrogenase (1%, transient)

Gastrointestinal: Abdominal pain (2%), diarrhea (4%), dyspepsia (2%), nausea (4%)

Hematologic & oncologic: Rectal hemorrhage (6%)

Hepatic: Abnormal liver function (1%; dose-related), increased serum alkaline phosphatase (1%, transient), increased serum transaminase (1%, transient)

Nervous system: Dizziness (1%), headache (3%)

Ophthalmic: Retinal hemorrhage (6%)

<1%, postmarketing, and/or case reports: Amblyopia, anemia, anorexia, colitis, conjunctivitis, constipation, dehydration, depression, diaphoresis, dyspnea, ecchymoses, emotional lability, epistaxis, esophagitis, flatulence, gastritis, gingival hemorrhage, hypersensitivity reaction, insomnia, leukopenia, maculopathy (Hanif 2019), optic neuritis, oral mucosa ulcer, pharyngitis, prolonged partial thromboplastin time, prolonged prothrombin time, pruritus, retinal pigment changes, rhinitis, skin photosensitivity, 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.

• Ocular effects: Pigmentary changes in the retina, including pigmentary maculopathy, have been reported with long-term use (≥3 years), but may occur with a shorter duration of use; cumulative dose may be a risk factor. Use with caution in patients with retinal pigment changes from other causes. Obtain a detailed ophthalmologic history prior to initiation of therapy; consider genetic testing in patients with a family history of hereditary pattern dystrophy. Retinal exams, including ocular coherence tomography and auto-fluorescence imaging, are recommended for all patients within 6 months of initiating therapy and periodically during treatment. A comprehensive baseline retinal exam, including color fundoscopic photography, ocular coherence tomography, and auto-fluorescence imaging, is recommended before initiating therapy in patients with preexisting ophthalmologic conditions. Risks and benefits of continuing treatment should be reevaluated if pigmentary changes in the retina develop; changes may be irreversible. Follow-up retinal examinations should be continued since retinal and vision changes may progress after discontinuation of therapy.

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.

Monitoring Parameters

Perform retinal exams for all patients within 6 months of initiating therapy and periodically during treatment; baseline retinal exam in patients with preexisting ophthalmologic conditions before initiating therapy.

Pregnancy Considerations

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

Patient Education

What is this drug used for?

• It is used to ease pain, swelling, and irritation of the bladder.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Upset stomach

• Dizziness

• Diarrhea

• Headache

• Hair loss

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Bleeding like throwing up or coughing up blood; vomit that looks like coffee grounds; blood in the urine; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a cause or that get bigger; or bleeding you cannot stop

• Changes in eyesight like trouble with reading, trouble getting used to low or dim light, or blurred eyesight

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.