Riluzole
Drug Info:
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Riluzole
Brand names: Rilutek®
Chemical formula:
- Espa�ol:
- Riluzol, Tableta oral
Riluzole Oral tablet
What is this medicine?
RILUZOLE (RIL yoo zole) slows down the progression of amyotrophic lateral sclerosis, also known as Lou Gehrig's disease.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•kidney disease
•liver disease
•an unusual or allergic reaction to riluzole, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take this medicine on an empty stomach, at least 1 hour before or 2 hours after meals. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
•allopurinol
•amitriptyline
•barbiturate, like phenobarbital
•caffeine
•carbamazepine
•certain antibiotics called quinolones
•methyldopa
•omeprazole
•phenacetin
•rifampin
•sulfasalazine
•tacrine
•theophylline
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. Contact your doctor or health care professional if your symptoms get worse or if you have a fever, chills, or other signs of infection.
Avoid alcohol and tobacco smoking while you are taking this medicine. Alcohol can increase the risk of liver damage. Tobacco smoking can decrease the effect of this medicine. Ask your doctor or health care professional for ways to help you stop smoking or drinking.
You may get dizzy or lose your balance. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•fever, chills or infection
•increased blood pressure
•tingling, pricking, or burning sensation around the mouth
•yellowing of the skin or eyes
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•cough
•diarrhea
•loss of appetite
•nausea, vomiting
•stomach pain
•weak or tired
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of reach of children.
Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Protect from light. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford A-Z of Medicinal Drugs:
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riluzole
A drug used in the treatment of motor neurone disease. It can only be used under specialist supervision. Riluzole is available as tablets on prescription only.
Side effects:
include weakness, nausea, vomiting, a fast heart rate, abdominal pain, dizziness, somnolence, tingling.
Precautions:
riluzole should not be taken by people with liver or kidney disease or by women who are pregnant or breastfeeding.
Proprietary preparation:
Rilutek.
| rifampicin, rifabutin, riboflavin | |
| rimexolone, risedronate sodium, risperidone |
Mosby's Dental Dictionary:
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riluzole
n
trade name: Rilutek; drug class: glutamate antagonist; action: inhibits presynaptic release of glutamic acid in central nervous system; use: treatment of amyotrophic lateral sclerosis (Lou Gehrig disease).
Wikipedia on Answers.com:
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Riluzole
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|---|---|
| Systematic (IUPAC) name | |
| 6-(trifluoromethoxy)benzothiazol-2-amine | |
| Clinical data | |
| Trade names | Rilutek |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a696013 |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 1744-22-5  |
| ATC code | N07XX02 |
| PubChem | CID 5070 |
| IUPHAR ligand | 2326 |
| DrugBank | DB00740 |
| ChemSpider | 4892 |
| UNII | 7LJ087RS6F |
| KEGG | D00775 |
| ChEMBL | CHEMBL744 |
| Chemical data | |
| Formula | C8H5F3N2OS |
| Mol. mass | 234.199 g/mol |
| SMILES | eMolecules & PubChem |
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 (what is this?) (verify) |
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Riluzole is a drug used to treat amyotrophic lateral sclerosis. It delays the onset of ventilator-dependence or tracheostomy in selected patients and may increase survival by approximately 3–5 months.
It is marketed by Sanofi-Aventis with the brand name Rilutek.
Riluzole preferentially blocks TTX-sensitive sodium channels, which are associated with damaged neurons.[1] This reduces influx of calcium ions and indirectly prevents stimulation of glutamate receptors. Together with direct glutamate receptor blockade, the effect of the neurotransmitter glutamate on motor neurons is greatly reduced.
However, the action of riluzole on glutamate receptors has been controversial, as no binding of the molecule has been shown on any known receptor.[2] In addition, as its antiglutamate action is still detectable in the presence of sodium channel blockers, it is also uncertain whether or not it acts via this way. Rather, its potent glutamate uptake activator activity seems to mediate many of its effects.[3] [4]
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Contents
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Studies of efficacy
A Cochrane Library review states a 9% gain in the probability of surviving one year. In secondary analyses of survival at separate time points, there was a significant survival advantage with riluzole 100 mg at six, nine, 12 and 15 months, but not at three or 18 months.[5] There was a small beneficial effect on both bulbar and limb function, but not on muscle strength. There were no data on quality of life, but patients treated with riluzole remained in a more moderately affected health state significantly longer than placebo-treated patients.
Clinical use
While riluzole has been proven to slow down ALS, patients do not report any subjective improvement. Approximately 10% of patients experience side effects such as nausea and fatigue which lead them to discontinue treatment. Safety monitoring includes regular liver function tests and people with liver disease such as hepatitis should be monitored especially carefully.
In the UK riluzole has been available through the NHS since 1997 at a standard dosage of 50 mg twice daily. There has been some evidence to show that higher doses might produce more significant improvements in ALS patients but at £5 a tablet it is at risk of being prohibitively expensive given the modest benefit to patients. One study in the Netherlands found that riluzole is metabolised differently by males and females, and its levels in plasma are decreased in patients who smoke cigarettes or take omeprazole.[6] [7]
A number of recent case studies have also indicated that riluzole may have clinical use in mood and anxiety disorders.[8] It has been shown to have antidepressant properties in the treatment of refractory depression[9] and as an anxiolytic in obsessive-compulsive disorder[10] and in GAD.[11]
References
- ^ Song JH, Huang CS, Nagata K, Yeh JZ, Narahashi T (1 August 1997). "Differential action of riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels". J Pharmacol Exp Ther. 282 (2): 707–14. PMID 9262334. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=9262334.
- ^ Wokke J (September 1996). "Riluzole". Lancet 348 (9030): 795–9. doi:10.1016/S0140-6736(96)03181-9. PMID 8813989.
- ^ Azbill RD, Mu X, Springer JE (July 2000). "Riluzole increases high-affinity glutamate uptake in rat spinal cord synaptosomes". Brain Res. 871 (2): 175–80. doi:10.1016/S0006-8993(00)02430-6. PMID 10899284. http://linkinghub.elsevier.com/retrieve/pii/S0006-8993(00)02430-6.
- ^ Dunlop J, Beal McIlvain H, She Y, Howland DS (1 March 2003). "Impaired spinal cord glutamate transport capacity and reduced sensitivity to riluzole in a transgenic superoxide dismutase mutant rat model of amyotrophic lateral sclerosis". J Neurosci. 23 (5): 1688–96. PMID 12629173. http://www.jneurosci.org/cgi/pmidlookup?view=long&pmid=12629173.
- ^ Miller RG, Mitchell JD, Lyon M, Moore DH (2007). Miller, Robert G. ed. "Riluzole for amyotrophic lateral sclerosis (ALS)/motor neuron disease (MND)". Cochrane Database Syst Rev (1): CD001447. doi:10.1002/14651858.CD001447.pub2. PMID 17253460.
- ^ van Kan HJ, Groeneveld GJ, Kalmijn S, Spieksma M, van den Berg LH, Guchelaar HJ (March 2005). "Association between CYP1A2 activity and riluzole clearance in patients with amyotrophic lateral sclerosis". Br J Clin Pharmacol 59 (3): 310–3. doi:10.1111/j.1365-2125.2004.02233.x. PMC 1884790. PMID 15752377. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1884790.
- ^ http://products.sanofi.us/rilutek/rilutek.html
- ^ Review of the Use of the Glutamate Antagonist Riluzole in Psychiatric Disorders and a Description of Recent Use in Childhood Obsessive-Compulsive Disorder. J Child Adolesc Psychopharmacol. 2010 August; 20(4): 309–315.
- ^ Zarate CA, Payne JL, Quiroz J, et al. (January 2004). "An open-label trial of riluzole in patients with treatment-resistant major depression". Am J Psychiatry 161 (1): 171–4. doi:10.1176/appi.ajp.161.1.171. PMID 14702270. http://ajp.psychiatryonline.org/cgi/content/full/161/1/171.
- ^ Coric V, Taskiran S, Pittenger C, et al. currently a study is underway at the NIH in Bethesda using riluzol for the treatment of OCD by Dr Grant (September 2005). "Riluzole augmentation in treatment-resistant obsessive-compulsive disorder: an open-label trial". Biol Psychiatry 58 (5): 424–8. doi:10.1016/j.biopsych.2005.04.043. PMID 15993857.
- ^ Mathew SJ, Amiel JM, Coplan JD, Fitterling HA, Sackeim HA, Gorman JM (December 2005). "Open-label trial of riluzole in generalized anxiety disorder". Am J Psychiatry 162 (12): 2379–81. doi:10.1176/appi.ajp.162.12.2379. PMID 16330605.
External links
- National Institute for Health and Clinical Excellence (NICE) guidelines for prescription of riluzole in the UK [1]
- Manufacturer's website [2]
- Riluzole (patient information)
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