Taltirelin-JG

Common name: taltirelin

Product name: Ceredist

All names: taltirelin tablets, taltirelin, Ceredist, Sawai

Indications:

For improving ataxia in patients with spinocerebellar degeneration

Usage and dosage:

Adults take 1 tablet twice a day, orally after breakfast and dinner, and can be increased or decreased appropriately according to age and symptoms.

Adverse reactions:

Digestive system reactions, including vomiting, nausea, and stomach discomfort

Taboo:

It is contraindicated in patients allergic to tapirelin.

Notes:

Use with caution in patients with impaired renal function.

Store:

Store at room temperature to avoid moisture after opening

Mechanism of action:

Pharmacological studies in animal CNS disease models have shown that THR can improve depression, circulatory shock, confusion, memory loss and motor skill impairment. However, clinical studies have shown that TRH has a short action time due to its rapid metabolic degradation in the body. In addition, the dose of TRH that produces endocrine effects is much lower than the effective dose on the CNS, so its clinical application is limited.

This product is a synthetic TRH analog. Pharmacological studies have shown that this product has strong and lasting multiple effects on the CNS via brain TRH receptors. The excitatory effect of this product on the CNS is 10-100 times stronger than that of TRH, and its duration of action is about 8 times longer than that of TRH. The affinity of this product for TRH receptor is about 1/11 of TRH, so the endocrine effect of this product is weaker than TRH, but this product is more stable than TRH in the body. In addition, the effect of this product on the release of thyroid stimulating hormone (TSH) is 1/6~1/11 of TRH. TSH release is regulated by a strong negative feedback system involving thyroid hormones. This negative feedback system also inhibits the potential endocrine effects of this product.

Safety and efficacy:

A 6-week randomized, double-blind, placebo-controlled, two-way crossover || phase clinical study was conducted in 60 patients with spinocerebellar degeneration. After 2 weeks of observation, the patients were divided into two groups. One group received 20 mg of this product twice a day for 2 weeks, and then received placebo for 2 weeks; the other group received placebo for 2 weeks, and then received this product for 2 weeks. The results showed that the overall improvement rate of the tartirelin tablets group was better than that of the placebo group (P=0.0394). This product group showed a tendency to be better than the placebo group in terms of neurological scores in the finger-to-nose test and tapping-point test. This product also improved spontaneous movements and overall mental state better than placebo (P=0.0448; P=0.0296, respectively).

In a double-blind randomized placebo-controlled clinical trial, 427 patients with spinocerebellar degeneration were randomly assigned to receive this product at 5 mg twice a day or placebo for 28 to 52 weeks. The overall improvement rate at 28 weeks was better than that of the placebo group (P<1.001). The cumulative change rate of this product group was 27.7%, while that of the placebo group was 47.1%. The overall improvement rate of ataxia in this product group was significantly better than that of the placebo group (P<0.004). The cumulative change rate of ataxia was 27.1% in the rosin group and 39.4% in the placebo group. The incidence rate of adverse reactions in this product group was 14.1%, which was almost the same as that in the placebo group.