Date of approval.
Date of revision.
Epalrestat Tablets Instructions
Please read the instructions carefully and use under the guidance of a physician.
[Drug Name].
Generic Name: Epalrestat Tablets
English Name: Epalrestat Tablets
Hanyu Pinyin：Yipasita Pian
Ingredients
The main ingredient of this product is Epalrestat
Its chemical name is: 5-[(1Z,2E)-2-methyl-3-phenylpropylene fork]-4-oxo-2-thio-3-thiazolidineacetic acid.
Its structural formula is as follows
Molecular formula: C15H13NO3S2
Molecular weight: 319.40
Properties
Appearance
This product is brown film-coated tablets, orange to orange-red after removing the coating.
Indications
Diabetic neuropathy.
Specification
Specification
50mg
Dosage and Administration
The usual adult dose is 50mg per dose, three times daily, taken orally before meals.
Adverse Reactions
The literature reports that through clinical trials and post-marketing surveillance, there were 119 cases (1.4%) and 149 adverse reactions (including abnormal clinical laboratory tests) in 8498 patients. Among them, there were 32 cases (0.4%) of abnormal liver function, mainly elevated AST (GOT) and ALT (GPT), 9 cases (0.1%) of abdominal pain, 9 cases (0.1%) of nausea, 6 cases (0.07%) of tiredness, etc.
Serious adverse reactions
Thrombocytopenia
Thrombocytopenia may occur (probability unknown), and the drug should be discontinued if it occurs.
Fulminant hepatitis, liver function impairment, jaundice, liver failure
Fulminant hepatitis (probability unknown), liver function abnormalities such as significant AST (GOT) and ALT (GPT) elevation (0.04%), jaundice (probability unknown), liver failure (probability unknown), etc. Discontinue the drug immediately after the occurrence of these adverse reactions.
Other adverse reactions
(1) Hypersensitivity: Occasional erythema, blistering, rash, itching.
(2) Liver: Occasionally elevated bilirubin, AST (GOT), ALT (GPT), and γ-glutamyl transferase (γ-GTP).
(3) Digestive system: occasional diarrhea, nausea, vomiting, abdominal pain, loss of appetite, abdominal fullness, stomach discomfort, constipation.
(4) Renal: occasional elevated creatinine, decreased urine output, frequent urination (probability unknown).
(5) Hematologic system: occasional anemia, leukopenia.
(6) Other: occasional lethargy, dizziness, headache, stiffness, weakness, palpitations, puffiness, swelling, pain, burning sensation in the extremities, numbness, hair loss, purple spots, elevated CK, fever, etc. (probability unknown).
Contraindication】
It is contraindicated for those who are hypersensitive to any of the ingredients in this product.
Precautions】
This product should be used under the guidance of a physician. The drug should be placed in a location inaccessible to children to prevent accidental ingestion by children.
This product is suitable for patients with glycosylated hemoglobin of 7.0% or higher. 3.
3. Some tests (e.g. bilirubin, ketone bodies) may be affected due to the possible maroon color of urine after taking this product.
4. Use with caution in patients with a history of allergy. In case of allergic manifestations, discontinue immediately and take appropriate treatment.
5. Patients who have not responded to 12 weeks of continuous use of this product should consider switching to another treatment.
Pregnant women and nursing mothers
There is no information on the safety of this product for use in women during pregnancy, therefore it should be used with extreme caution in women during pregnancy and only when the benefits outweigh the risks. Animal studies have shown that epalrestat can be excreted through breast milk, so women who are breastfeeding should avoid using this product.
Pediatric Use]
The safety and efficacy of this product in children have not been established.
Geriatric use
In elderly patients with altered physiological functions, appropriate dosage reduction should be considered when using this product.
Drug Interactions
Not yet known.
Drug Overdose
No overdose has been reported.
Pharmacology and Toxicology
Pharmacological effects
Epalrestat is a reversible non-competitive inhibitor of aldose reductase with selective inhibitory effect on aldose reductase. Clinical studies have shown that epalrestat can inhibit the accumulation of sorbitol in erythrocytes of patients with diabetic peripheral neuropathy and improve the autonomic symptoms and neurological dysfunction of patients compared with the control group. The results of animal tests showed that epalrestat significantly inhibited the accumulation of sorbitol in the sciatic nerve, erythrocytes and retina of the diabetic model rats, and improved the motor nerve conduction velocity and autonomic function; in terms of neuromorphology, epalrestat improved the abnormal axonal flow, increased the density of myelinated nerve fibers in the sciatic nerve, the thickness of the myelin sheath of the peroneal nerve, the axonal area and the axonal cylindrical rate; in addition, epalrestat also In addition, epalrestat also improved the blood flow to the sciatic nerve and increased the inositol content in the model animals.
Toxicological studies
Genotoxicity: The results of Epalrestat Ames test, CHL cell chromosome aberration test and mouse micronucleus test were all negative.
Reproductive toxicity: Fertility and early embryonic development toxicity test, embryo-fetal development toxicity test and perinatal toxicity test were not abnormal in rats given epalrestat 20, 100 and 500 mg/kg by gavage; in rabbits given 20, 100, 250 and 500 mg/kg by gavage, abortion and complete fetal absorption were observed at 500 mg/kg dose. The incidence of miscarriage and complete fetal absorption increased at 500 mg/kg.
Carcinogenicity: No significant increase in tumor incidence was observed in mice given Epalrestat 300, 800, 2000ppm by adulteration for 18 months and in rats given Epalrestat 500, 1500, 5000ppm by adulteration for 24 months.
Pharmacokinetics]
According to the literature, the peak blood concentration (3.9µg/mL) was reached after 1 hour of oral administration of 50mg in healthy adults. Animal experiments have confirmed that the product is mainly distributed in the gastrointestinal tract, liver and kidneys, with about 8% excreted in the urine and 80% excreted in the feces after 24 hours.
Storage
Storage
Keep it under shade and sealed.
Package
Packaging
Packed in aluminum foil and PVC solid pharmaceutical rigid tablets, 10 tablets per plate, 1 plate per box; 9 tablets per plate, 2 plates per box.
Available
Efficacy
Period】
12 months
Execution Standard
Approval Number
Manufacturer
Company Name: Yangtze River Pharmaceutical Group Nanjing Hailing Pharmaceutical Co.
Production Address: No. 9, Xianlin Avenue, Qixia District, Nanjing
Zip code: 210049
Telephone number: 025-83505999-6895
Website：http：//www.hailingyy.com