How Do Glutamate Inhibitors Work?

Glutamate inhibitors or glutamate antagonist drugs inhibit the action of neurotransmitter glutamate on neurons and are used to treat amyotrophic lateral sclerosis (ALS), also known as motor neuron disease or Lou Gehrig’s disease, caused by loss of or damage to motor neurons.

Riluzole, a glutamate inhibitor drug that belongs to the benzothiazole class is a Food and Drug Administration-approved medication for the treatment of ALS.

Glutamate is an abundant, powerful excitatory neurotransmitter present almost in all neural synapses in the central nervous system and plays an essential role in the functioning of the brain. Glutamate levels need to be well regulated, as excessive exposure to glutamate may be toxic to neurons and may damage them leading to ALS. The mode of action of riluzole is unknown. According to its pharmacological properties:

• Riluzole may block the voltage-dependent sodium channels associated with damaged neurons.
• Riluzole may prevent glutamate release from presynaptic neurons.
• Riluzole directly inhibits the activity of ionotropic receptors such as kainate receptors also known as kainic acid receptors and N-methyl-D-aspartate receptors from binding with glutamate.

Glutamate inhibitors are used to treat ALS.

Side effects of glutamate inhibitors may include:

• Nausea and vomiting
• Headache
• Dizziness
• Weakness
• Decreased lung function
• Abdominal pain
• Hepatitis (inflammation of the liver)
• Elevated liver enzymes
• Pancreatitis (swelling and inflammation of the pancreas)
• Muscular weakness
• Increased heart rate
• Increased blood pressure
• Insomnia
• Urinary tract infections
• Vertigo (spinning sensation)

Other rare side effects of glutamate inhibitors may include:

• Neutropenia (low neutrophil count)
• Anaphylaxis (life-threatening allergic reactions)
• Angioedema (swelling under the skin or mucous membrane because of accumulation of fluid)

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of glutamate inhibitors include:

• Exservan
• Rilutek
• Riluzole
• Tiglutik