Riluzole
Riluzole Uses, Dosage, Side Effects, Food Interaction and all others data.
The mode of action of riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect:
An inhibitory effect on glutamate release (activation of glutamate reuptake),Inactivation of voltage-dependent sodium channels,Ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors.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. The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective.
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. The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective.
| Trade Name | Riluzole |
| Availability | Prescription only |
| Generic | Riluzole |
| Riluzole Other Names | Riluzol, Riluzole, Riluzolum |
| Related Drugs | edaravone, Radicava, Radicava ORS, Rilutek, Exservan, Tiglutik |
| Weight | 50mg/10ml, 50mg |
| Type | Oral suspension, oral tablet |
| Formula | C8H5F3N2OS |
| Weight | Average: 234.198 Monoisotopic: 234.007468097 |
| Protein binding | 96% bound to plasma proteins, mainly to albumin and lipoprotein over the clinical concentration range. |
| Groups | Approved, Investigational |
| Therapeutic Class | Neurodegenerative Disease Drugs / Neuromuscular Disorder Drugs |
| Manufacturer | Ranbaxy (UK) Limited a Sun Pharmaceutical Company |
| Available Country | United Kingdom, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Riluzole is used for the treatment of amyotrophic lateral sclerosis (ALS).
Riluzole is also used to associated treatment for these conditions: Amyotrophic Lateral Sclerosis (ALS)
How Riluzole works
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 receptors.
Dosage
Riluzole dosage
The recommended dosage for Riluzole is 50 mg taken orally twice daily. Riluzole should be taken at least 1 hour before or 2 hours after a meal.Measure serum aminotransferases before and during treatment with Riluzole
Side Effects
The following adverse reactions are described below and elsewhere in the labeling: Hepatic Injury, Neutropenia, Interstitial lung disease
Precaution
Hepatic Injury: Cases of drug-induced liver injury, some of which were fatal, have been reported in patients taking Riluzole. Asymptomatic elevations of hepatic transaminases have also been reported, and in some patients have recurred upon rechallenge with Riluzole.
In clinical studies, the incidence of elevations in hepatic transaminases was greater in Riluzoletreated patients than placebo-treated patients. The incidence of elevations of ALT above 5 times the upper limit of normal (ULN) was 2% in Riluzole-treated patients. Maximum increases in ALT occurred within 3 months after starting Riluzole. About 50% and 8% of Riluzoletreated patients in pooled Studies 1 and 2, had at least one elevated ALT level above ULN and above 3 times ULN, respectively
Monitor patients for signs and symptoms of hepatic injury, every month for the first 3 months of treatment, and periodically thereafter. The use of Riluzole is not recommended if patients develop hepatic transaminases levels greater than 5 times the ULN. Discontinue Riluzole if there is evidence of liver dysfunction (e.g., elevated bilirubin).
Neutropenia: Cases of severe neutropenia (absolute neutrophil count less than 500 per mm3) within the first 2 months of Riluzole treatment have been reported. Advise patients to report febrile illnesses.
Interstitial Lung Disease: Interstitial lung disease, including hypersensitivity pneumonitis, has occurred in patients taking Riluzole. Discontinue Riluzole immediately if interstitial lung disease develops.
Interaction
Strong to moderate CYP1A2 inhibitors: Coadministration may increase Riluzole-associated adverse reactions
Strong to moderate CYP1A2 inducers: Coadministration may result in decreased efficacy
Hepatotoxic drugs: Riluzole-treated patients that take other hepatotoxic drugs may be at increased risk for hepatotoxicity
Food Interaction
- Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.
Riluzole Drug Interaction
Unknown: amphetamine / dextroamphetamine, lorazepam, diphenhydramine, heparin, clonazepam, escitalopram, lithium, mirabegron, dextromethorphan / quinidine, acetaminophen / oxycodone, vitamin a topical, bioflavonoids, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, ranitidine, sertraline
Riluzole Disease Interaction
Moderate: alcohol, liver disease, neutropenia, renal dysfunction
Elimination Route
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%.
Half Life
The mean elimination half-life of riluzole is 12 hours (CV=35%) after repeated doses.
Pregnancy & Breastfeeding use
Pregnancy: Based on animal data, may cause fetal harm
Lactation: It is not known if riluzole is excreted in human milk. Riluzole or its metabolites have been detected in milk of lactating rat. Women should be advised that many drugs are excreted in human milk and that the potential for serious adverse reactions in nursing infants from Riluzole is unknown.
Contraindication
Riluzole is contraindicated in patients with a history of severe hypersensitivity reactions to riluzole or to any of its components (anaphylaxis has occurred)
Acute Overdose
Reported symptoms of overdose following ingestion of Riluzole ranging from 1.5 to 3 grams (30 to 60 times the recommended dose) included acute toxic encephalopathy, coma, drowsiness, memory loss, and methemoglobinemia. No specific antidote for the treatment of Riluzole overdose is available.
Storage Condition
Store at controlled room temperature, 20°C to 25°C, and protect from bright light.
Innovators Monograph
You find simplified version here Riluzole
Riluzole contains Riluzole see full prescribing information from innovator Riluzole Monograph, Riluzole MSDS, Riluzole FDA label
FAQ
What is Riluzole used for?
Riluzole is a medication used to slow the progression of amyotrophic lateral sclerosis (ALS).Riluzole is the only drug to prolong survival for amyotrophic lateral sclerosis
How safe is Riluzole?
The Riluzole is generally very safe if monitored correctly.
How does Riluzole work?
Riluzole works by blocking the release of glutamate.
What are the common side effects of Riluzole?
Common side effects of Riluzole are include:
- Bladder pain
- bloody or cloudy urine
- blurred vision
- chills
- cough
- dark urine
- diarrhea
- difficult, burning, or painful urination
- fast, pounding, or irregular heartbeat or pulse
- fever
- frequent urge to urinate
- general feeling of discomfort or illness
- headache
- increased cough
- itching skin
- joint pain
- loss of appetite
- lower back or side pain
- muscle aches and pains
- nausea
- nervousness
- persistent loss of appetite or weight loss
- pounding in the ears
- right upper quadrant tenderness
- runny nose
- shivering
- slow heartbeat
- sore throat
- trouble sleeping
- unusual tiredness or weakness
- vomiting
- yellow eyes or skin
Is Riluzole safe during pregnancy?
Riluzole may harm an unborn baby. Use effective birth control to prevent pregnancy, and tell your doctor if you become pregnant. Ask a doctor if it is safe to breastfeed while using this medicine.
Is Riluzole safe during breastfeeding?
There are no adequate studies in women for determining infant risk when using Riluzole during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Can I drink alcohol with Riluzole?
Avoid drinking alcohol. It may increase your risk of liver damage while taking Riluzole. This medication may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.
Can I drive after taking Riluzole?
This drug may make you dizzy or drowsy.Do not drive, use machinery, or do anything that needs alertness until you can do it safely.
When Is the best taken of Riluzole?
Riluzole should be taken on an empty stomach. Take it at least 1 hour before or 2 hours after meals. This medicine works best if there is a constant amount in the blood.
How can I take Riluzole?
Riluzole usually is taken on an empty stomach twice a day, every 12 hours.
How long does it take for Riluzole to work?
It is working behind the scenes to prolong your survival and slow the progression of ALS. The initial clinical trials showed a survival benefit of about 3 months. However, more recent data suggest that the survival benefit may be as much as 12 months, especially for younger patients.
Does Riluzole cause liver damage?
The severity of liver injury from Riluzole ranges from minor, transient elevations in serum aminotransferase levels to acute hepatic injury with jaundice and possible to acute liver failure.
Does Riluzole raise blood pressure?
Blood pressures were significantly higher in Riluzole treated patients than in controls with ALS.Riluzole treatment may be associated with mild blood pressure elevations.
Who should not take Riluzole?
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
What happen If I miss a dose of Riluzole?
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Skip the missed dose and take your next dose at the regular time. Do not use extra medicine to make up for a missed dose.
How long does Riluzole stay in my system?
Given the known half-life of Riluzole(9–15 hours) and the delay of emergence of amnesia, most of the Riluzole should have been out of our patient's system by the time the symptoms emerged, which raises the possibility that she may have been a slow metabolizer of the drug.
How long should I take Riluzole?
The initial clinical trials showed a survival benefit of about 3 months.
Can Rilutek be crushed?
Swallow the tablet whole. Do not break, crush, or chew it.
Can you overdose on Riluzole?
Overdose symptoms may include drowsiness, confusion, problems with thinking or memory, coma, tremors, or blue lips or fingers. Avoid smoking. Smoking cigarettes may make riluzole less effective.
