爱泌罗(Elmiron)中文说明书

Elmiron is a low molecular weight heparin-like compound that has anticoagulant and fibrinolytic effects. The mechanism of Elmiron in treating interstitial cystitis is unclear.

Elmiron indications

Elmiron is indicated for the relief of bladder pain or discomfort associated with interstitial cystitis.

Elmiron usage and dosage

1. Recommended dose

300 mg/day, one 100 mg capsule each time, three times a day.

2. How to take

Capsules should be taken with water, and should be taken at least 1 hour before or 2 hours after a meal.

3. Post-medication evaluation

Patients receiving Elmiron should be re-evaluated after 3 months. If no improvement is seen and there are no limiting adverse events, they can continue to take Elmiron for another 3 months.

4. Tips for long-term treatment

However, for patients whose pain has not been significantly improved by Almiro for more than 6 months, the clinical value and risk indications of continuing treatment with this drug are still unclear.

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.

Contraindications of Elmiron

It is contraindicated in patients with a known history of allergy to Elmiron, structurally related compounds or excipients.

Elmiron Precautions

1. Retinal pigment changes

Retinal pigment changes have been found in long-term use of Elmiron (reported in the literature as pigmentary maculopathy).

Patients with existing ophthalmic diseases should undergo a comprehensive baseline retinal examination before starting treatment, such as color fundus photography, optical coherence tomography (OCT) and autofluorescence imaging.

All patients are recommended to have a baseline retinal examination within 6 months of starting treatment and to have regular reexaminations during continued treatment.

If retinal pigment changes occur, the risks and benefits of continued treatment should be reassessed, as these changes may be irreversible.

Given that retinal and visual acuity changes may progress even after discontinuation of treatment, follow-up retinal examinations should be continued.

2. Risks related to anticoagulation

Elmiron is a weak anticoagulant (1/15 of the activity of heparin), and patients who undergo invasive procedures or have signs/symptoms of potential coagulopathy or other increased bleeding risks (due to the use of other therapies such as coumarin anticoagulants, heparin, t-PA, streptokinase, high-dose aspirin, or nonsteroidal anti-inflammatory drugs) should be evaluated for bleeding.

Patients with medical conditions such as aneurysms, thrombocytopenia, hemophilia, gastrointestinal ulcers, polyps or diverticula should undergo necessary medical evaluation before starting use of Almirol.

3. Hair loss

Related to Elmiron and heparin products, hair loss begins within the first 4 weeks of treatment. 97% of reported cases of hair loss are alopecia areata, limited to a single area of ​​the scalp.

4. Medication in patients with hepatic impairment

Elmiron has not been studied in patients with hepatic impairment because there is evidence that the liver is involved in the elimination of Elmiron, and impairment of liver function may affect its pharmacokinetics. Caution should be exercised when using almirol in this patient population.

Adverse reactions of Elmiron

1. Incidence (1% to 4%)

Alopecia (4%), diarrhea (4%), nausea (4%), headache (3%), rash (3%), indigestion (2%), abdominal pain (2%), abnormal liver function (1%), dizziness (1%).

2. Incidence rate (≤1%)

(1) Digestive system

Vomiting, oral ulcers, colitis, esophagitis, gastritis, flatulence, constipation, anorexia, and gum bleeding.

(2), Blood system

Anemia, ecchymoses, prolonged prothrombin time, prolonged partial thromboplastin time, leukopenia, and thrombocytopenia.

(3), allergic reaction

Allergic reaction, photosensitivity reaction.

(4) Respiratory system

Pharyngitis, rhinitis, epistaxis, and dyspnea.

(5), skin and appendages

Itching and urticaria.

(6), special senses

Conjunctivitis, tinnitus, optic neuritis, amblyopia, retinal hemorrhage.

Elmiron Medication for Special Populations

1. Pregnancy

Adequate and well-controlled studies have not been conducted in pregnant women because animal studies do not always predict human responses and this drug should be used during pregnancy only when clearly needed.

2. Breastfeeding women

It is not clear whether Almerol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when giving Almerol to lactating women.

3. Pediatric use

The safety and effectiveness in pediatric patients under 16 years of age have not been determined.

Elmiron drug interactions

In one study, healthy subjects took 100 mg of Elmiron capsules or placebo every 8 hours for 7 days and titrated with warfarin to an international normalized ratio (INR) of 1.4-1.8.

The results showed that the pharmacokinetic parameters of R-warfarin and S-warfarin were similar in the presence and absence of allerol. The INR values ​​of warfarin + placebo and warfarin + allerol were comparable.

Elmiron overdose

There have been no reports of Elmiron overdose. Based on the pharmacodynamic properties of the drug, toxicity is likely to manifest as anticoagulation, bleeding, thrombocytopenia, abnormal liver function and gastric discomfort.

While gastric lavage is performed on patients with acute drug overdose, they should also be closely observed and given corresponding symptomatic and supportive treatment.

Mechanism of action of Elmiron

The mechanism by which Elmiron works in patients is unclear. In preliminary clinical models, Elmiron adheres to the mucosa of the bladder wall.

Elmiron may act as a buffer to control cell permeability and prevent irritating solutes in urine from reaching cells.

Elmiron Pharmacokinetics

1. Absorption

In a clinical pharmacology study, healthy female volunteers took a single oral dose of 300 mg or 450 mg of Elmiron containing radiolabeled drugs under fasting conditions. The median time for the peak concentration of plasma radioactivity was approximately 2 hours after taking the drug (range 0.6-120 hours).

Based on urinary excretion of radioactivity, an average of approximately 6% of a radiolabeled oral dose is absorbed and enters the systemic circulation.

Food effect: In clinical trials, Almiro was taken with water and was taken 1 hour before or 2 hours after a meal. The effect of food on the absorption of Almiro is unclear.

2. Distribution

Preclinical studies on parenterally administered radiolabeled Aimero showed that it is distributed in the urothelium of the genitourinary tract, with smaller amounts in the liver, spleen, lungs, skin, periosteum and bone marrow. In animals, it has low permeability to red blood cells.

3. Metabolism

The absorbed Amirol is partially desulfated and metabolized in the liver and spleen, and partially depolymerized and metabolized in the kidneys, producing a large number of metabolites. The desulfation and depolymerization will reach saturation with continued administration.

4. Excretion

After oral administration of 300 mg or 450 mg of almirol containing radiolabeled drugs to healthy subjects, the average half-life of plasma radioactivity was 27 hours and 20 hours respectively.

The majority of oral doses of almirol (average 84% in the 300 mg group and 58% in the 450 mg group) were excreted unchanged in the feces.

An average of 6% of the oral dose is excreted in the urine, mostly as desulfated and depolymerized metabolites. Only a small fraction of the administered dose (0.14% on average) is recovered in the urine as intact drug.

Elmiron Pharmacokinetics in Special Populations

The pharmacokinetics of Elmiron have not been studied in elderly patients or patients with hepatic and renal insufficiency.

Elmiron supply specifications

Elmiron is a white opaque hard gelatin capsule, printed with the words "BNP7600", containing 100 mg of Elmiron, and the supply specification is a bottle of 100 capsules.

Elmiron Storage

Store at 20°C to 25°C (68°F to 77°F); excursions allowed between 15°C and 30°C (59°F to 86°F).

Please keep out of the reach of children.

Warm Tips

1. Patients are advised to read the FDA-approved Patient Medication Guide. Patients should strictly follow the dosage and frequency prescribed by the prescription, and should not exceed the dosage or take it more frequently.

2. Patients should be informed that any changes in vision should be reported promptly and evaluated. It is recommended that all patients undergo retinal examinations, including optical coherence tomography (OCT) and autofluorescence imaging, within six months of starting almirol and periodically during long-term treatment.