Riluzole

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Riluzole is a medication used to treat amyotrophic lateral sclerosis (ALS), also known as Lou Gehrig's disease. It is one of the few treatments available that can extend the life expectancy of patients with ALS. Riluzole works by inhibiting the release of glutamate, a neurotransmitter that is believed to contribute to the degeneration of motor neurons in ALS.

Mechanism of Action

Riluzole is classified as a glutamate antagonist. It inhibits the release of glutamate by blocking voltage-gated sodium channels on neurons. This action helps to protect motor neurons from excitotoxicity, a process where excessive glutamate causes neuronal damage and death. By reducing glutamate levels, riluzole helps to slow the progression of ALS.

Indications

Riluzole is primarily indicated for the treatment of amyotrophic lateral sclerosis. It is not a cure for ALS but has been shown to extend survival by several months. The medication is typically prescribed to patients who have been diagnosed with ALS and are experiencing symptoms such as muscle weakness and difficulty speaking or swallowing.

Dosage and Administration

Riluzole is administered orally, usually in the form of a tablet. The recommended dosage is 50 mg taken twice daily. It is important for patients to take riluzole on an empty stomach, either one hour before or two hours after meals, to ensure proper absorption.

Side Effects

Common side effects of riluzole include:

• Nausea
• Dizziness
• Fatigue
• Diarrhea

Serious side effects can include liver damage, which is why regular monitoring of liver function tests is recommended during treatment. Symptoms of liver damage may include jaundice, dark urine, and persistent nausea or vomiting.

Contraindications

Riluzole is contraindicated in patients with a known hypersensitivity to the drug or any of its components. It should also be used with caution in patients with liver disease or elevated liver enzymes.

Pharmacokinetics

Riluzole is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1 to 1.5 hours. It is extensively metabolized in the liver, primarily by the cytochrome P450 enzyme CYP1A2. The metabolites are then excreted in the urine.

History

Riluzole was approved by the Food and Drug Administration (FDA) in 1995 for the treatment of ALS. It was the first drug to be approved for this condition and remains one of the few options available for ALS patients.

Research

Ongoing research is exploring the potential use of riluzole in other neurodegenerative diseases, such as Huntington's disease and Alzheimer's disease. Studies are also investigating the combination of riluzole with other therapies to enhance its efficacy in treating ALS.

See Also

• Amyotrophic lateral sclerosis
• Glutamate
• Neurodegenerative disease
• Motor neuron

External Links

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Riluzole

Drug Information
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Identifiers		Chemical Data Molecular Weight