RILUTEK 50MG TABLET

Indications

• Amyotrophic lateral sclerosis (ALS)
• Motor neuron disease

Dosage

Adults: The usual dosage is 50 mg orally twice daily.

Mechanism of action

Riluzole acts by several mechanisms, including the inhibition of glutamate release, inactivation of voltage-dependent sodium channels, and interference with intracellular processes following the binding of excitatory amino acids to their receptors. These actions may contribute to its neuroprotective effects in conditions where excitotoxicity is a factor.

Pharmacodynamics

As a member of the benzothiazole class, riluzole exhibits neuroprotective properties and is specifically indicated for patients with ALS, where it has been shown to prolong survival and improve time to tracheostomy. Riluzole's pharmacological effects may relate to its ability to counteract glutamate-induced neuronal damage, which is implicated in the pathogenesis of ALS and other neurodegenerative disorders.

Pharmacokinetics

Riluzole is absorbed after oral administration and is extensively metabolized in the liver. It has a half-life of approximately 12 hours. The drug is excreted primarily as metabolites in the urine. Caution is advised in patients with hepatic impairment, as this may lead to increased drug exposure.

Adverse effects

• Neutropenia
• Dizziness
• Drowsiness
• Headache
• Nausea
• Abdominal pain
• Diarrhoea

Interactions

• Mexiletine: Unknown (increases exposure)
• Osilodrostat: Unknown (increases exposure)
• Ciprofloxacin: Unknown (increases exposure)
• Rucaparib: Unknown (increases exposure)
• SSRIs: Unknown (increases exposure)
• Vemurafenib: Unknown (increases exposure)
• Fluvoxamine: Unknown (increases exposure)

Precautions

• Perform chest radiography if symptoms such as dry cough or dyspnoea develop.
• Monitor white blood cell counts in febrile illness.
• Patients should recognize signs of neutropenia and seek medical attention if fever occurs.
• Use with caution in patients with hepatic impairment (avoid due to increased exposure).
• Use with caution in patients with renal impairment (avoid if possible).
• Dizziness or vertigo may affect the performance of skilled tasks.

Pregnancy

Avoid-no information available.

Breast-feeding

Avoid-no information available.

Storage

Store in a cool, dry place away from direct sunlight.

Formulations

• Riluzole 50 mg tablets
• Riluzole 5 mg per 1 ml oral suspension

Mechanism of action

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.

Pharmacodynamics

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 <i>in vivo</i> 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.