Riluzole PMCS 50 mg, 56 tablets: profile, composition and research

Reference page for Riluzole PMCS 50 mg, 56 tablets. Active substance: Рилузол / Riluzole.

Key facts

What riluzole is

Riluzole is an active substance used in amyotrophic lateral sclerosis (ALS). The disease is also known as Charcot disease or motor neuron disease: it progressively destroys motor nerve cells, and muscle weakness follows.

The medicine is one of the few agents able to influence the course of the disease rather than a single symptom. The PMCS pack contains 56 film-coated tablets, each with 50 mg of the active substance.

Besides riluzole the tablet contains excipients: calcium phosphate, microcrystalline cellulose, colloidal silicon dioxide, croscarmellose sodium and magnesium stearate. The coating is made of hypromellose, macrogol 6000 and titanium dioxide. This design protects the active substance and controls its release in the gastrointestinal tract.

How riluzole works

The glutamate problem

Motor neurons communicate through signalling molecules, and the main excitatory messenger in that system is glutamate. Normally it is released in measured amounts and cleared quickly from the synaptic cleft. In ALS the balance breaks down and glutamate accumulates in excess.

What happens to the neuron

Excess glutamate overstimulates the cell. Calcium ions flood in, oxidative cascades start, mitochondria suffer, and the motor neuron dies. The phenomenon is called glutamate excitotoxicity.

What the medicine does

Riluzole weakens that cascade: it reduces the release of glutamate from nerve endings and blocks voltage-gated sodium channels, lowering membrane excitability. It cannot halt the process completely, but its intensity is reduced.

Approved uses

Riluzole is registered for the treatment of amyotrophic lateral sclerosis in adults. That is its only approved indication.

Controlled trials assessed how the medicine affects survival and the rate at which motor function is lost. According to that work the gain is measured in weeks or months and does not mean recovery of abilities already lost. Patients and their families are better off understanding this in advance, so that expectations stay realistic.

Riluzole does not restore dead neurons and does not stop the disease. The decision to prescribe it, the duration of the course and the assessment of benefit belong to a neurologist.

Monitoring during treatment

The most frequent laboratory change on riluzole is a rise in liver enzyme activity, alanine aminotransferase above all. The change is usually transient, yet monitoring of blood biochemistry remains mandatory throughout the whole course.

Among common adverse events the labelling lists asthenia, somnolence, dizziness, tachycardia, paraesthesia, nausea, vomiting, diarrhoea and abdominal pain. Less often anaemia, a fall in neutrophil count and persistent headache are noted. In rare cases severe reactions are possible, including liver injury and pancreatitis.

Dizziness can affect the ability to drive and to operate machinery. That question is worth discussing with a doctor before treatment begins.

Published research

Primary sources, verified against PubMed:

• Riluzole for amyotrophic lateral sclerosis (ALS)/motor neuron disease (MND)., PubMed 22419278 (Cochrane Database Syst Rev, 2012).
• A controlled trial of riluzole in amyotrophic lateral sclerosis. ALS/Riluzole Study Group., PubMed 8302340 (N Engl J Med, 1994).
• Riluzole for the treatment of amyotrophic lateral sclerosis., PubMed 32847483 (Neurodegener Dis Manag, 2020).

Listed for reference. Publication of a study is not a claim about this particular product.

Precautions

• This is a prescription medicine. Prescribing, dosing and monitoring belong to a physician.
• Regular monitoring of liver enzymes is mandatory during treatment. Any sign of liver injury should be reported to a doctor without delay.
• Weakness, somnolence and dizziness are possible. Until the reaction to the medicine is clear, driving and operating machinery are best avoided.
• Use during pregnancy or breastfeeding is discussed with a doctor individually.
• Liver or kidney disease requires a physician's assessment before treatment starts.
• Tell your doctor about every other medicine you take: interactions are possible.

Frequently asked