Riluzole

234.2

234.20

1592732-453-0

7LJ087RS6F

759823|753433

DTXSID3045192

C47704

N07XX02|N - Nervous system

2934999090

76.4

3.6

white solid

1.6±0.1 g/cm3

117-119 °C

296.3°C at 760 mmHg

133.0±30.1 °C

1.615

DMSO: ≥25 mg/mL

Store at RT

0.00145mmHg at 25°C

II

6.1

UN 2811 6.1/PG 3

3

25

45

DL2830000

T,Xi

Irritant

P301 + P310

H301

|Danger|H301 (96.3%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P321, P330, P405, and P501|Aggregated GHS information provided by 135 companies from 6 notifications to the ECHA C&L Inventory.

Serum aminotransferase elevations occur in approximately up to 12% of patients on long term riluzole therapy, but elevations above 3 times the upper limit of normal (ULN) occur in less than 3% of patients. These elevations are usually mild-to-moderate in severity and are rarely associated with symptoms. Most elevations resolve spontaneously, but persistent or marked elevations require drug discontinuation or dose modification. Routine monitoring of serum aminotransferase levels is recommended for the first 6 months of therapy. Clinically apparent liver injury due to riluzole is rare, but several cases have been reported, arising after 1 to 12 months of therapy and characterized by a hepatocellular or mixed pattern of serum enzyme elevations. Immunoallergic and autoimmune features were uncommon. Most cases were mild to moderate in severity and recovery was rapid upon drug discontinuation, but evidently fatal cases have been reported to the sponsor.

96% bound to plasma proteins, mainly to albumin and lipoprotein over the clinical concentration range.

For the treatment of amyotrophic lateral sclerosis (ALS, Lou Gehrig's Disease)|FDA Label|Rilutek is indicated to extend life or the time to mechanical ventilation for patients with amyotrophic lateral sclerosis (ALS).Clinical trials have demonstrated that Rilutek extends survival for patients with ALS.Survival was defined as patients who were alive, not intubated for mechanical ventilation and tracheotomy-free.There is no evidence that Rilutek exerts a therapeutic effect on motor function, lung function, fasciculations, muscle strength and motor symptoms.Rilutek has not been shown to be effective in the late stages of ALS.Safety and efficacy of Rilutek has only been studied in ALS. Therefore, Rilutek should not be used in patients with any other form of motor-neurone disease.|Riluzole Zentiva is indicated to extend life or the time to mechanical ventilation for patients with amyotrophic lateral sclerosis (ALS).Clinical trials have demonstrated that Riluzole Zentiva extends survival for patients with ALS. Survival was defined as patients who were alive, not intubated for mechanical ventilation and tracheotomy-free.There is no evidence that Riluzole Zentiva exerts a therapeutic effect on motor function, lung function, fasciculations, muscle strength and motor symptoms. Riluzole Zentiva has not been shown to be effective in the late stages of ALS.Safety and efficacy of Riluzole Zentiva has only been studied in ALS. Therefore, Riluzole Zentiva should not be used in patients with any other form of motor-neurone disease.

Riluzole is a neuroprotective agent used for therapy of amyotrophic lateral sclerosis. Riluzole is associated with a low rate of serum aminotransferase elevations during therapy and has been linked to rare instances of clinically apparent, acute liver injury.

Amyotrophic Lateral Sclerosis Agents

Riluzole, a member of the benzothiazole class, is indicated for the treatment of patients with amyotrophic lateral sclerosis (ALS). Riluzole extends survival and/or time to tracheostomy. It is also neuroprotective in various in vivo experimental models of neuronal injury involving excitotoxic mechanisms. The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective.

Drugs used to prevent SEIZURES or reduce their severity. (See all compounds classified as Anticonvulsants.)|Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists. (See all compounds classified as Excitatory Amino Acid Antagonists.)|Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids. (See all compounds classified as Neuroprotective Agents.)

Riluzole is well-absorbed (approximately 90%), with average absolute oral bioavailability of about 60% (CV=30%). A high fat meal decreases absorption, reducing AUC by about 20% and peak blood levels by about 45%.

Riluzole is extensively metabolized to six major and a number of minor metabolites, which have not all been identified to date. Metabolism is mostly hepatic, consisting of cytochrome P450–dependent hydroxylation and glucuronidation. CYP1A2 is the primary isozyme involved in N-hydroxylation; CYP2D6, CYP2C19, CYP3A4, and CYP2E1 are considered unlikely to contribute significantly to riluzole metabolism in humans.|Riluzole has known human metabolites that include 4-hydroxy-riluzole, 5-hydroxy-riluzole, 7-hydroxy-riluzole, and N-Hydroxyriluzole.

The mean elimination half-life of riluzole is 12 hours (CV=35%) after repeated doses.

The mode of action of riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release (activation of glutamate reuptake), 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors.

2 Amino 6 trifluoromethoxybenzothiazole

Human drugs -> Rilutek -> EMA Drug Category|Other nervous system drugs -> Human pharmacotherapeutic group|Human drugs -> Riluzole Zentiva -> EMA Drug Category|Human drugs -> Rare disease (orphan)|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients