Riluzole: Formula, Indications, Mechanism of Action, Dosage, Side Effects, Warnings, Contraindications and Interactions

It is a drug that lowers the levels of glutamate in the body, it is an amino acid that acts on the nerves that send messages from the brain to the muscles.

Patients with amyotrophic lateral sclerosis often have very high glutamate levels , which end up damaging nerve cells.

Riluzole is indicated to prolong life or delay the use of assisted mechanical ventilation in patients with amyotrophic lateral sclerosis.

Riluzole is a glutamate antagonist, used as an anticonvulsant, and is used to prolong survival in patients with amyotrophic lateral sclerosis.

The definition of survival is a living patient, not intubated for assisted mechanical ventilation and not tracheostomized.

Therapeutic action on motor functions, respiratory function, fasciculations, muscle strength and motor symptoms has not been demonstrated.

Riluzole does not show any beneficial effect in the advanced stages of amyotrophic lateral sclerosis.

Chemical formula

  • C8H5F3N2OS.


Oral tablet of 50 mg.


For the treatment of amyotrophic lateral sclerosis (Lou Gehrig’s disease).

Mechanism of action

The mode of action of riluzole is unknown.

Its pharmacological properties include the following, some of which may be amyotrophic lateral sclerosis.

It has an inhibitory effect on the release of glutamate (activation of glutamate reuptake), it achieves the inactivation of voltage-gated sodium channels.

It has the ability to interfere with intracellular events that follow the binding of the transmitter to excitatory amino acid receptors.

Although the pathogenesis of amyotrophic lateral sclerosis is not fully elucidated, it appears that glutamate, the central excitatory neurotransmitter of the central nervous system, plays a role in the cell death associated with the disease.


The recommended dose of riluzole for adults or in geriatric patients is 100 mg per day or 50 mg every twelve hours.

Side effects

In clinical trials conducted in riluzole-treated patients with amyotrophic lateral sclerosis, the most frequently reported adverse reactions were asthenia, nausea, and abnormal liver parameters.

Riluzole should be stopped and your doctor called right away if you have a serious side effect, such as:

  • Nausea, stomach pain, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).
  • Fever, chills, body aches, and flu symptoms.
  • Coughing up yellow or green mucus.
  • Stabbing pain in the chest, dry cough, shortness of breath, feeling short of breath.

Less serious side effects may include:

  • Dizziness
  • Muscular stiffness.
  • Weakness, drowsiness
  • Numbness or tingling sensation in or around your mouth.
  • Mild nausea, diarrhea, stomach pain, constipation .
  • Headache.

Warnings and Contraindications

Liver disorders

Riluzole should be administered with caution in patients with abnormal liver function or in patients with elevated serum transaminase values.

Renal insufficiency

The use of riluzole in patients with renal impairment is not recommended due to the absence of repeated dose studies in these types of patients.

Pediatric use

The use of riluzole in children is not recommended, since there are no data on the efficacy and safety of the use of the drug in neurodegenerative diseases.


Onset of febrile illness should result in blood count control and discontinuation of riluzole treatment in case of neutropenia.

Interstitial lung disease

Serious cases of interstitial lung disease have been reported in patients treated with riluzole.

In the case of signs suggestive of interstitial disease, lung disease such as diffuse, bilateral pulmonary opacities, dry cough, dyspnea , riluzole should be discontinued immediately.

In most of the reported cases, the symptoms disappear, after discontinuation of the product and under symptomatic treatment.

Lactation and pregnancy

Riluzole is contraindicated in women who are breast-feeding. It is unknown whether riluzole passes into human breast milk.

The physician should be informed if the patient is pregnant.


This medication should not be used if you are allergic to riluzole or any other medications.

Caffeine and alcohol

Caffeine can cause too much riluzole to build up in your body.

Alcohol can cause liver damage if taken together with riluzole.


There are a wide variety of medications that interact with riluzole such as:

  • Acetaminofen (Tylenol).
  • Alopurinol (Zyloprim).
  • Amitriptyline (Vile Amyotrophic Lateral Sclerosis, Vanatrip).
  • Auranofin (Ridaura).
  • Cancer drugs.
  • Metildopa (Aldomet).
  • Omeprazol (Prilosec).
  • Sulfasalazina (azulfidina).
  • Theophylline (Elixophyllin, Theo-24, Theochron, Uniphyl, and others).
  • Medicines for tuberculosis.
  • Pills for birth control or other hormones.
  • Methotrexate (Rheumatrex, Trexall).
  • Angiotensin converting enzyme inhibitors such as benazepril (Lotensin), enalapril (Vasotec), lisinopril (Prinivil, Zestril), quinapril (Accupril), ramipril (Altace) among others.
  • Antibiotic as ciprofloxacin (Cipro), dapsona, erythromycin (EES, EryPed, Ery-Tab, Erythrocin).
  • Levofloxacin (Levaquin), norfloxacin (Noroxin), ofloxacin (Floxin) or rifampicin (Rifater, Rifadin, Rifamate).
  • Antimycotic drugs such as fluconazole (Diflucan), itraconazole (Sporanox) or ketoconazole (Extina, Ketozole, Nizoral, Xolegal).
  • Medications for cholesterol, such as comoniacin (Advicor, Niaspan, Niacor, Slo-niacin, among others), atorvastatin (Lipitor), simvastatin (Zocor, Simcor, Vytorin), lovastatin (Mevacor), pravastatin (Pravachol) among others.
  • Medicines such as abacavir, lamivudine, zidovudine (Trizivir), lamivudine (Combivir, Epivir), nevirapine (Viramune), tenofovir (Viread), zidovudine (Retrovir).
  • Nonsteroidal anti-inflammatory drugs such as ibuprofen (Motrin, Advil), naproxen (Aleve, Naprosyn), diclofenac (Cataflam, Voltaren), etodolac (Lodine), indomethacin (Indocin), ketoprofen (Orudis), and others.
  • Seizure medications, such as carbamazepine (Carbatrol, Tegretol), phenytoin (Dilantin), felbamate (Felbatol), valproic acid (Depakene).