Pentosan Polysulfate Sodium

Pentosan Polysulfate Sodium is approved for use in the following clinical indications

• Interstitial cystitis

Pentosan polysulfate is a sulfated pentosyl polysaccharide used to treat bladder pain and discomfort due to interstitial cystitis.

• Interstitial cystitis

Adult Oral Dose: 100 mg 3 times daily.

Pediatric Oral Dose:

Adolescents ≥16 years: Oral: 100 mg 3 times daily.

• 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.

• 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.

• Alopecia (Hair loss)

The use of Pentosan Polysulfate Sodium may cause hair loss in some people. Consult your doctor if you have any concerns.

Common

• Alopecia, diaphoresis, skin rash, Endocrine & metabolic: Increased gamma-glutamyl transferase, increased lactate dehydrogenase, Abdominal pain, diarrhea, dyspepsia, nausea ,Rectal hemorrhage, Abnormal liver function, increased serum alkaline phosphatase, increased serum transaminase , Depression, dizziness, emotional lability, headache, insomnia, Ecchymoses, pruritus, skin photosensitivity, urticaria, Anorexia, colitis, constipation, esophagitis, flatulence, gastritis, gingival hemorrhage, oral mucosa ulcer, vomiting, Anemia, leukopenia, prolonged partial thromboplastin time, prolonged prothrombin time, thrombocytopenia, Hypersensitivity reaction, Amblyopia, conjunctivitis, optic neuritis, retinal hemorrhage, Tinnitus, Dyspnea, epistaxis, pharyngitis, rhinitis.

Rare

• Ophthalmic: Macular degeneration, maculopathy (including pigmentary maculopathy with long-term use), retinal pigment changes, retinal toxicity (including retinal dystrophy and injury).

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

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

The common side effects of Pentosan Polysulfate Sodium include the following

• Common side effects

Hair loss, diarrhea, upset stomach, heartburn, headache, rash, stomach pain, difficulty falling asleep or staying asleep, moodiness, dizziness.

• Rare side effects

Unusual bruising or bleeding, nosebleed, heavy gum bleeding, black and tarry stools, red blood in stools, bloody vomit.

• Pregnancy

Pregnancy Category B

Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women.

• 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.

• Pediatric Use

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

• Geriatric Use

Information not available

Symptoms: Anticoagulation, bleeding, thrombocytopenia, liver function abnormalities and gastric distress.

• Pharmacodynamic

The mechanism by which pentosan polysulfate sodium achieves its effects in patients is unknown. In preliminary clinical models, pentosan polysulfate sodium adhered to the bladder wall mucosal membrane. The drug may act as a buffer to control cell permeability preventing irritating solutes in the urine from reaching the cells.

• Pharmacokinetics

Absorption

Pentosan sodium is absorbed from the GI tract. Time taken to reach peak plasma concentration is 2 hours. It has bioavailability of approximately 6%.

Metabolism and Excretion

Extensively metabolised in the liver and spleen by partial desulfation and in the kidney by partial depolymerisation. Mainly excreted via faeces (58-84%, as unchanged drug) in urine (6%, mainly as desulfated and depolymerised metabolites).