Entacapone Tablets

This product belongs to catechol-O-methyltransferase (COMT) inhibitors. It is a reversible, specific, and mainly peripheral COMT inhibitor, used simultaneously with levodopa preparations. This product reduces the metabolism of levodopa to 3-oxo-methyldopa (3-OMD) by inhibiting the COMT enzyme, which increases the bioavailability of levodopa and the total amount of levodopa available in the brain. This effect has been confirmed in clinical trials. This product mainly inhibits COMT in peripheral tissues. The COMT inhibitory effect in erythrocytes is closely related to the plasma concentration of this product, which reflects the reversibility of COMT inhibitory effect.

The main ingredients and chemical names of this product are: diacetylaminoacetic acid ethylenediamine

This product is an orange-brown film-coated tablet, which appears yellow after removing the coating.

This product can be used as an adjunct to the standard drugs levodopa/benserazide or levodopa/carbidopa to treat Parkinson's disease that cannot be controlled by the above drugs and end-of-dose phenomenon (symptom fluctuations).

Administer 200 mg (1 tablet) of this product each time you take levodopa/dopa decarboxylase inhibitors. The maximum recommended dose is 200 mg (1 tablet), 10 times a day, i.e. 2 g of this product.

Common adverse reactions include diarrhea, worsening Parkinson's disease symptoms, dizziness, abdominal pain, insomnia, dry mouth, fatigue, hallucinations, constipation, dystonia, dystonia, hyperkinesia, headache, leg cramps, confusion, nightmares, falls, orthostatic hypotension, vertigo, and tremor.

Patients with known allergies to this product or any other component; patients with impaired liver function are contraindicated. This product is not suitable for patients with pheochromocytoma because it increases the risk of hypertensive crisis. Patients with a history of malignant neuroleptic syndrome (NMS) and/or non-traumatic rhabdomyolysis are contraindicated.

Precautions for children: Not yet clear. Precautions for pregnancy and lactation: Not yet clear. Precautions for the elderly: There is still a lack of safety research data on the use of this product in elderly patients.

Concomitant use of non-selective MAO (MAO-A and MAO-B) inhibitors (e.g., phenelzine, tranylcypromine) with tamoxifen is contraindicated. Similarly, concomitant use of a selective MAO-A inhibitor plus a selective MAO-B inhibitor with tamoxifen is contraindicated. tamoxifen can be used in combination with selegiline (a selective MAO-B inhibitor), but the latter should not exceed 10 mg per day. Due to its mechanism of action, tamoxifen may interfere with the metabolism of catechol-containing drugs and enhance their effects. Therefore, tamoxifen should be administered with caution to patients receiving drugs metabolized by COMT, such as rimiterol, isoproterenol, epinephrine, norepinephrine, dopamine, dobutamine, alpha;-methyldopa, and apomorphine. No interaction between tamoxifen and carbidopa was observed at the recommended dose. No pharmacokinetic interaction studies between tamoxifen and benserazide were conducted. In single-dose studies in healthy volunteers, no interaction between tamoxifen and imipramine or between tamoxifen and moclobemide was observed. Similarly, no interaction between this product and selegiline was observed in repeated dosing studies in patients with Parkinson's disease. However, clinical experience with the simultaneous use of this product with several drugs, including MAO-A inhibitors, tricyclic antidepressants, norepinephrine reuptake inhibitors such as desipramine, maprotiline, venlafaxine, and drugs containing catechol structures that are metabolized by COMT is still limited. If this product is used in combination with any of the above drugs, patients should be carefully monitored (see [Precautions]). This product can form chelates with iron in the gastrointestinal tract. The interval between the administration of this product and iron preparations is at least 2-3 hours (see [Adverse Reactions]). This product binds to human albumin binding site II, which is also bound to some other drugs such as diazepam and ibuprofen. No clinical studies on interactions with diazepam and non-steroidal anti-inflammatory drugs have been conducted. In vitro experiments showed that no significant displacement reactions occurred at therapeutic drug concentrations.

Store at room temperature. Valid for 3 years.

100 ml: 0.6 g of ethylenediamine diacetate and 0.9 g of sodium chloride

Tentative 18 months