A glutamate antagonist (receptors, glutamate)
Rilunorm(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 in vivo experimental models of neuronal injury involving excitotoxic mechanisms.
Psychiatric use
A number of recent case studies have indicated that riluzole may have clinical use in mood and anxiety disorders.It has been shown to have antidepressant properties in the treatment of refractory depression and act as an anxiolytic in obsessive-compulsive disorder and in generalized anxiety disorder.
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 the survival of patients with amyotrophic lateral sclerosis
Absorption: Riluzole is well-absorbed (approximately 90%), with average absolute oral bioavailability of about 60% (CV=30%). A high fat meal decreases absorption, reducing AUC by about 20% and peak blood levels by about 45%.
Protein binding: 96% bound to plasma proteins, mainly to albumin and lipoprotein over the clinical concentration range.
Metabolism:Riluzole is extensively metabolized to six major and a number of minor metabolites, which have not all been identified to date. Metabolism is mostly hepatic, consisting of cytochrome P450–dependent hydroxylation and glucuronidation. CYP1A2 is the primary isozyme involved in N-hydroxylation; CYP2D6, CYP2C19, CYP3A4, and CYP2E1 are considered unlikely to contribute significantly to riluzole metabolism in humans.
Half life: The mean elimination half-life of riluzole is 12 hours (CV=35%) after repeated doses.
(R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Riluzole. 3-isobutyl-1-methyl-7H-xanthine The serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Riluzole. 4-Methoxyamphetamine The risk or severity of adverse effects can be increased when Riluzole is combined with 4-Methoxyamphetamine. 6-O-benzylguanine The serum concentration of 6-O-benzylguanine can be increased when it is combined with Riluzole. 7-Deazaguanine The serum concentration of 7-Deazaguanine can be increased when it is combined with Riluzole. 7-Nitroindazole The risk or severity of adverse effects can be increased when Riluzole is combined with 7-Nitroindazole.
7,9-Dimethylguanine The serum concentration of 7,9-Dimethylguanine can be increased when it is combined with Riluzole. 8-azaguanine The serum concentration of 8-azaguanine can be increased when it is combined with Riluzole. 8-chlorotheophylline The serum concentration of 8-chlorotheophylline can be increased when it is combined with Riluzole. 9-Deazaguanine The serum concentration of 9-Deazaguanine can be increased when it is combined with Riluzole. Take on an empty stomach 1 hour before or 2 hours after meals.
Side effect:Dizziness, lightheadedness, drowsiness, tiredness, nausea, vomiting, diarrhea, loss of appetite, stomach pain, or numbness/tingling around the mouth may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Tell your doctor right away if you have any serious side effects, such as: signs of infection (such as sore throat that doesn't go away, fever, chills
Precautions:Before taking riluzole, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease.
This drug may make you dizzy or drowsy. Alcohol or marijuana can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana.
Smoking may affect the level of this drug in your blood. Tell your doctor if you smoke or use nicotine or if you stop smoking.

Kidney and liver function decline as you grow older. This medication is removed by the kidneys and liver. Therefore, the elderly may be more sensitive to the side effects of the drug.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.
It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

What should I know regarding pregnancy, nursing and administering Riluzole to children or the elderly?Interactions: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (such as prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
Some products that may interact with this drug are: other drugs that may cause liver problems (such as allopurinol, methyldopa, sulfasalazine), drugs affecting liver enzymes that remove riluzole fromyourbody (such as amitriptyline, caffeine, omeprazole, rifampin, tacrine, quinolone antibiotics such as ciprofloxacin)