Comfora

Non-brittle hard gelatin capsules no. 2, blue cap, white body with white to pale yellow powder.
Each hard gelatin capsule contains: Pentosan Polysulfate Sodium 100 mg.

Pharmacotherapeutic group: Urologicals, other urologicals.
Pharmacology: Pharmacodynamics: Mechanism of action: The hypothetic mechanism of action of pentosan polysulfate sodium includes a local effect in the bladder after systemic administration and excretion into the urine by binding of glycosaminoglycans to the deficient mucous of the bladder. This binding of glycosaminoglycans to the bladder mucous reduces bacterial adherence to the inner surface of the bladder and in consequence the incidence of infections is reduced as well. It is hypothesized, that a potential barrier function of pentosan polysulfate sodium instead of the damaged urothelial mucus might play a role as well the anti-inflammatory activity of pentosan polysulfate sodium.
Pharmacokinetics: Absorption: Less than 10% of orally administered pentosan polysulfate sodium are slowly absorbed from the gastrointestinal tract and are available in systemic circulation in the form of unchanged pentosan polysulfate sodium or its metabolites. All studies describe very low systemic availability of unchanged pentosan polysulfate sodium after oral administration. Overall, the reported systemic bioavailability after oral administration of pentosan polysulfate sodium is below 1%.
Distribution: In healthy volunteers, a single parenteral administration of radioactively labelled pentosan polysulfate sodium leads to a progressive uptake of total radioactivity by the liver, spleen, and kidney (50 min after 1 mg/kg I.V.: 60% of the dose in the liver, 7.7% in the spleen; 3 h post dosing: 60% in the liver plus spleen, and 13% in the bladder).
Biotransformation: Pentosan polysulfate sodium is metabolised extensively by desulfation in liver and spleen and depolymerisation in the kidney.
Elimination: The apparent plasma half-life of pentosan polysulfate sodium depends on the route of administration. While pentosan polysulfate sodium is rapidly cleared from circulation of I.V. administration, the apparent plasma half-life after oral administration is in the range of 24-34 hours. Accordingly, oral administration of pentosan polysulfate sodium 3-times daily is expected to lead to accumulation of pentosan polysulfate sodium over the first 7 days of administration (accumulation factor 5-6.7). After oral administration unabsorbed pentosan polysulfate sodium is excreted predominantly unchanged in the feces. About 6% of the administered dose of pentosan polysulfate sodium were excreted via urine after desulfation and depolymerisation.

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

Adults: The recommended dose of pentosan polysulfate sodium is 300 mg/day taken as one 100 mg capsule orally three times daily.
Response to treatment with pentosan polysulfate sodium should be reassessed every 3 months. In case no improvement is reached 6 months after treatment initiation, treatment with pentosan polysulfate sodium should be stopped. In responders, pentosan polysulfate sodium treatment should be continued chronically as long as the response is maintained.
Special populations: Pentosan polysulfate sodium has not been specifically studied in special patient populations like elderly, male patients or patients with renal or hepatic impairment. No dose adjustment is recommended for these patients.
Pediatric population: The safety and efficacy of pentosan polysulfate sodium in children and adolescent below 18 years has not been established. No data are available.
Method of administration: The capsules should be taken with water at least 1 hour before meals or 2 hours after meals.
Or as prescribed by the physician.

In the case of an accidental overdose, patients should be evaluated for potential adverse effects of pentosan polysulfate sodium like gastrointestinal symptoms or bleeding. In case of adverse reactions, treatment might be paused until the symptoms abate and treatment should be continued at the recommended dose after a critical balancing of the risks thereafter.

Hypersensitivity to the active substance or to any of the excipients.
Due to the weak anticoagulant effect of pentosan polysulfate sodium, pentosan polysulfate capsule must not be used in patients who actively bleed. Menstruation is no contraindication.

Bladder pain syndrome is a diagnosis of exclusion and other urologic disorders should be eliminated by the prescriber, such as urinary tract infection or bladder cancer. Pentosan polysulfate sodium is a weak anticoagulant. Patients undergoing invasive procedures or having signs/symptoms of underlying coagulopathy or other increased risk of bleeding (due to treatment with other medicinal products influencing coagulation such as anticoagulants, heparin derivatives, thrombolytic or antiplatelet agents including acetylsalicylic acid, or nonsteroidal anti-inflammatory medicinal products should be evaluated for hemorrhagic events. Patients who have a history of heparin or pentosan polysulfate sodium induced thrombocytopenia should be carefully monitored when treated with pentosan polysulfate sodium.
Hepatic or renal insufficiency: Pentosan polysulfate sodium capsule has not been studied in patients with hepatic or renal insufficiency. Because there is evidence of hepatic and renal contribution to the elimination of pentosan polysulfate sodium, hepatic or renal impairment may have an impact on the pharmacokinetics of pentosan polysulfate sodium. Patients with relevant hepatic or renal insufficiency should be carefully monitored when treated with pentosan polysulfate sodium.
Retinal Pigmentary Changes: Pigmentary changes in the retina, reported in the literature as pigmentary maculopathy, have been identified with long-term use of Pentosan polysulfate sodium.

Pregnancy: There are no data from the use of pentosan polysulfate sodium in pregnant women. Animal studies with respect to reproductive toxicity were not conducted.
Pentosan polysulfate sodium capsules is not recommended during pregnancy.
Breastfeeding: It is unknown whether pentosan polysulfate sodium or metabolites are excreted in human milk. A risk to the newborns/infants cannot be excluded.
Therefore, pentosan polysulfate sodium should not be used during breastfeeding.
Fertility: No information on a potential impact of pentosan polysulfate sodium on fertility is available.

Summary of the safety profile: The following section lists adverse events reported in the literature from clinical studies with pentosan polysulfate sodium. The potential relatedness between these adverse events and the treatment with pentosan polysulfate sodium was not discussed in the respective publications.
The most common adverse events reported from the clinical studies are headache, dizziness and gastrointestinal events like diarrhea, nausea, abdominal pain and rectal bleeding.
The adverse events reported under treatment with pentosan polysulfate sodium were comparable to those reported under treatment with placebo in regards to quality and quantity.
Tabulated summary of adverse events: Adverse events are listed as follows by MedDRA body system organ class and by frequency. very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000); not known (cannot be estimated from available data). (See table.)

Click on icon to see table/diagram/image

A study in healthy subjects revealed no pharmacokinetic or pharmacodynamic interactions between therapeutic doses of warfarin and pentosan polysulfate sodium. No further interaction studies have been performed.
Due to the weak anticoagulant effect of pentosan polysulfate sodium, patients who are concomitantly treated with anticoagulants, heparin derivatives, thrombolytic or antiplatelet agents including acetylsalicylic acid, or nonsteroidal anti-inflammatory medicinal products should be evaluated for any hemorrhagic event in order to adapt the dose if needed.

Store at temperatures not exceeding 30°C.

Other Drugs Acting on the Genito-Urinary System

G04BX15 - pentosan polysulfate sodium ; Belongs to the class of other urologicals.

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