Riluzole Tablets

The pharmacokinetics of riluzole were evaluated in healthy male volunteers after single oral doses of 25 to 300 mg and repeated oral doses of 25 to 100 mg twice daily. The increase in plasma concentration levels was linear with the dose. Its pharmacokinetic properties were non-dose dependent. When repeated doses were administered (50 mg riluzole tablets, twice daily, for a ten-day course of treatment), riluzole prototype accumulated in plasma to twice the single dose and reached steady state within 5 days. Absorption: Riluzole is rapidly absorbed after oral administration and reaches maximum plasma concentration within 60 to 90 minutes (Cmax=173plusmn;72(sd)ng/ml). Approximately 90% of the dose is absorbed, and the absolute bioavailability is 60plusmn;18%. When riluzole is taken with a high-fat meal, its absorption rate and extent of absorption are reduced. (Cmax decreased by 44%, and the area under the curve decreased by 17%). Distribution: Riluzole is widely distributed in the body and can pass the blood-brain barrier. The volume of distribution of riluzole is approximately 245 plus mn; 69 liters (3.4 liters/kg body weight). The protein binding rate of riluzole is approximately 97%, mainly bound to plasma albumin and lipoproteins. Metabolism: Riluzole is mainly present in plasma in its original form and is extensively metabolized by cytochrome P450 and then glycosylated. In vitro experiments using prepared human livers showed that cytochrome P4501A2 is the main isoenzyme involved in the metabolism of riluzole. The metabolites in urine are 3 phenolic derivatives, 1 ureido derivative and unchanged riluzole. The identified and unbound metabolites do not show the pharmacodynamic properties of riluzole in animals and have not been studied in humans. Excretion: The excretion half-life ranges from 9 to 15 hours. Riluzole is mainly excreted in urine. The total excretion rate in urine is 90% of the dose. Glucuronic acid derivatives account for more than 85% of the metabolites in urine. Only 2% of the dose of riluzole is present in urine in its original form. The pharmacokinetic parameters of riluzole in elderly healthy volunteers did not change, so there are no special requirements for the use of riluzole in the elderly population. The metabolism of this drug in patients with impaired renal function is not significantly different from that in healthy adults, but the AUC of patients with mild and moderate chronic liver dysfunction increased by 1.7 times and 3 times, respectively, suggesting that riluzole should not be used in patients with liver disease and transaminase levels 3 times higher than the upper limit of normal values.

The main ingredient of this product is riluzole, and its chemical name is: 2-chloro-6-trifluoromethoxybenzothiazole.

This product is white or off-white tablets.

For the treatment of patients with amyotrophic lateral sclerosis, it can prolong survival and/or delay the need for tracheotomy.

Oral administration, 50 mg (1 tablet) at a time, twice a day. Increasing the daily dosage will not increase the efficacy of the drug, but will increase adverse reactions. If you miss a dose, take the next tablet as planned. The drug should be taken 1 hour before or 2 hours after a meal to reduce the effect of food on the bioavailability of riluzole.

Common adverse reactions to this product are fatigue, stomach discomfort, and increased plasma transaminase levels. Other adverse reactions are less common. Neutropenia is occasionally seen. This product may cause other adverse reactions not listed here. If you experience any changes in your health while taking this product, please inform your doctor or pharmacist.

Those who are allergic to this product and its main ingredients. Those with abnormal liver function or abnormally elevated transaminase levels. Those who are pregnant or breastfeeding.

Precautions for children: There is no research data on the use of riluzole tablets in children. Precautions for pregnancy and lactation: Pregnant and lactating women are prohibited. Precautions for the elderly: The medication for elderly patients is the same as that for healthy adults.

Cytochrome P4501A2 is the main metabolizing enzyme of this drug. CYP1A2 inhibitors (caffeine, phenacetin, theophylline, amitriptyline and quinolones) may reduce the clearance of this drug. CYP1A2 inducers (smoking, rifampicin, omeprazole) may increase the clearance of this drug.

Store in a dark, dry and cool place. Valid for 2 years.

50mg

24 months

Jiangsu Nhwa Pharmaceutical Co., Ltd.

• Founded in:

  1999-03-29

• Address:

  No. 18, Yangshan Road, Xuzhou Economic and Technological Development Zone

• Tax NO.:

  913203001363846728

• Registered Funds:

  1016.176792 million yuan

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