爱泌罗(Elmiron)的详细说明书：作用与功效,用法用量,副作用,注意事项

Elmiron is a semi-synthetic low molecular weight heparin-like drug that is a urinary protective agent and its structure is similar to naturally occurring glycosaminoglycans.

Elmiron effects and efficacy

Interstitial Cystitis

Elmiron is used to relieve bladder pain or discomfort associated with interstitial cystitis.

Orphan drug qualification: The US FDA has granted orphan drug qualification for the treatment of this disease.

Elmiron usage and dosage

1. Route of administration

Oral administration: It needs to be taken with water, and it should be taken at least 1 hour before or 2 hours after a meal.

2. Dosage instructions

This product is provided in the form of sodium pentosan polysulfate, and the dosage is calculated on a salt basis.

3. Adult dosage

100 mg each time, 3 times a day, for 3 months.

4. Treatment evaluation

If no improvement is seen after 3 months and there are no dose-limiting adverse reactions, treatment can be continued for another 3 months.

The manufacturer points out that if pain is not relieved after 6 months, the clinical benefits and risks of continued treatment are unclear. However, long-term clinical research data shows that continued treatment for 1 to 2 years can improve overall symptoms, such as pain, urgency, frequency of urination, and nocturia.

Some clinicians recommend a dose of 200 mg twice daily, which appears to be effective and helps improve patient compliance.

The pictures come from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Elmiron dosage for special groups

1. People with liver insufficiency

No specific dosage adjustment recommendations.

2. Patients with renal insufficiency

No specific dosage adjustment recommendations.

3. Elderly patients

No specific dosage adjustment recommendations.

Contraindications of Elmiron

It is contraindicated in persons with known allergies to pentosan polysulfate sodium, structurally related compounds, or any ingredients in the preparation.

Precautions for Elmiron

1. Effects on the blood system

Elmiron is a weak anticoagulant, and bleeding complications such as rectal bleeding and ecchymosis, epistaxis, and gum bleeding have been reported.

Patients at higher risk of bleeding need to be evaluated, including those undergoing invasive procedures, those with symptoms or signs of coagulopathy, and those taking concomitant medications that affect hemostasis.

There have been reports showing that subcutaneous, intramuscular or sublingual administration of almirol in different dosage forms may cause delayed immunoallergic thrombocytopenia.

Symptoms are similar to those of heparin-induced thrombocytopenia, including thrombotic and bleeding manifestations.

It should be used with caution in patients with a history of heparin-induced thrombocytopenia, and patients with thrombocytopenia should be carefully evaluated before starting treatment.

Thrombocytopenia, prothrombin time (PT), and partial thromboplastin time (PTT) prolongation have been reported in patients with abnormal liver function test results.

2. Comorbid diseases

Patients with diseases such as aneurysm, hemophilia, gastrointestinal ulcers, polyps or diverticula need to be carefully evaluated before starting treatment.

3. Liver effects

About 1.2% of patients experience mild and usually transient increases in serum aminotransferase, alkaline phosphatase, γ-glutamyl transpeptidase and lactate dehydrogenase concentrations (less than 2.5 times the upper limit of normal).

These abnormalities usually occur within 3 to 12 months after starting treatment and are usually not accompanied by jaundice or other clinical signs and symptoms. These increases may remain unchanged or rarely progress as the medication is continued.

4. Hair loss

Hair loss has been reported, mainly alopecia areata (confined to a single area of ​​the scalp), which may occur within 4 weeks of starting treatment.

Elmiron medication for special groups

1. Pregnancy period

The pregnancy classification is Category B.

2. Lactation period

It is not clear whether pentosan polysulfate sodium is secreted with breast milk. Breastfeeding women should use with caution.

3. Pediatric use

The safety and effectiveness of the drug for patients under 16 years of age have not been established.

4. Patients with hepatic insufficiency

It should be used with caution. It has not been studied in patients with hepatic insufficiency. Hepatic insufficiency may alter pharmacokinetics because allerol is metabolized by the liver.

Common adverse reactions of Elmiron

Rectal bleeding, hair loss, diarrhea, nausea, headache, bloody stools, rash, indigestion, abdominal pain, abnormal liver function, dizziness, and bruises.

Elmiron drug interactions

Drugs that affect hemostasis

Combined use may increase the risk of bleeding, and signs of bleeding need to be monitored during combined use.

Elmiron Pharmacokinetics

1. Absorption

Bioavailability: After oral administration of radiolabeled sodium pentosan polysulfate (solution), approximately 6% is absorbed by the system, and the median time to peak plasma radioactivity is 2 hours (range 0.6 to 120 hours).

Onset of effect: Pain relief in patients with early or mild interstitial cystitis occurs within 6 to 8 weeks; most patients with moderate to severe interstitial cystitis experience pain relief after about 6 months.

Duration: Pain relief can last for more than 29 months in some patients.

Food effects: The effect of food on the absorption of sodium pentosan polysulfate is unclear. In clinical trials, it is required to take it with water and take it 1 hour before or 2 hours after a meal.

2. Distribution

Scope: In animals, it is distributed in the urothelium of the genitourinary tract, and less commonly in the liver, spleen, lungs, skin, periosteum and bone marrow. Small amounts enter red blood cells in animals.

Whether it is secreted with breast milk is unclear.

3. Metabolism

Orally absorbed sodium pentosan polysulfate is partially desulfated in the liver and spleen and depolymerized in the middle of the kidney to form a large number of metabolites. Continued administration may result in saturation of desulfation and depolymerization pathways.

4. Elimination pathways

After oral administration of a dose of 300 or 450 mg of radioactive labeling (solution), 84% or 58% respectively are excreted in the original form in the feces; about 6% are excreted in the urine, mainly as desulfated and depolymerized metabolites.

Half-life: The mean half-life of plasma radioactivity after oral administration of a radiolabeled 300 or 450 mg dose (solution) is 27 hours or 20 hours, respectively.

Elmiron storage conditions

Oral capsules: Store at 15–30°C.

Mechanism of action of Elmiron

As a semi-synthetic low molecular weight heparin-like drug, Elmiron is a urinary protective agent with a structure similar to natural glycosaminoglycans.

The main cause of interstitial cystitis may be a defect in the glycosaminoglycan layer of the bladder mucus, leading to increased permeability of the bladder epithelium. This permeability allows irritating urine solutes to enter the interstitial tissue and cause tissue damage.

Although the mechanism of action of Almerol in the treatment of interstitial cystitis is not fully elucidated, the drug appears to replenish the defective mucus (glycosaminoglycan) layer and restore bladder integrity (by adhering to the bladder surface); it acts as a buffer to control cell permeability and prevent irritating solutes from contacting epithelial cells.

After oral administration, it is a weak anticoagulant (activity equivalent to 1/15 of heparin), which may prolong bleeding time.

Parental administration (no parenteral preparations are available in the United States) can inhibit the production of factor X.

In vitro studies show inhibition of thrombin-induced platelet aggregation.

Warm Tips

1. You must take Amirol according to the prescription, including not changing the frequency of medication on your own.

2. It needs to be taken with water and taken at least 1 hour before or 2 hours after a meal.

3. In case of accidental overdose, contact the emergency room and/or poison control center immediately.

4. This medicine can only be used by the patient himself and only for the prescribed indications, and must not be given to others.

5. Patients need to be informed of the risk of bleeding.

6. Before any surgery, you should consult your doctor whether you need to stop taking medication.

7. Female patients should inform their doctor if they are pregnant, planning to become pregnant or breastfeeding.

8. The doctor needs to be informed of existing or planned concomitant drugs (such as prescription drugs such as warfarin and heparin or over-the-counter drugs such as certain non-steroidal anti-inflammatory drugs), as well as concomitant diseases (such as liver disease, diseases requiring surgery).