Rilutek (riluzole)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Riluzole is an antiglutamate agent that acts in the CNS.
Riluzole, a synthetic aryl-substituted benzothiazolamine, is an antiglutamate agent that acts in the CNS. It has been suggested that the motor neuron degeneration associated with amyotrophic lateral sclerosis (ALS) may be related to accumulation of excitatory amino acids (EAAs), principally glutamate, at synapses in the CNS and resultant ''excitotoxicity'' and cell death.
The precise mechanism of action of riluzole in patients with ALS has not been fully elucidated but appears to involve interference with the effects mediated by EAAs in the CNS, possibly through inhibition of glutamic acid release, blockade or inactivation of voltage-dependent sodium channels, and/or activation of a G-protein-dependent signal transduction pathway. While some data also suggest that riluzole may act via noncompetitive blockade of EAA receptors, the drug has not been shown to bind to any known glutamate receptor. Riluzole has exhibited neuroprotective properties in vitro and in vivo in animals, including inhibition of neuronal toxicity associated with exposure to EAAs or cerebrospinal fluid from ALS patients, and inhibition of neuronal toxicity associated with anoxia or focal or global ischemia.
Riluzole prolonged survival in a study in a transgenic mouse model of ALS but did not delay onset of the disease.
Riluzole exhibits dose-proportional pharmacokinetics over the dosage range of 25-100 mg every 12 hours. The oral bioavailability of the drug is approximately 60%. Similar pharmacokinetics were observed following intragastric administration (via feeding tube) and oral administration of the oral suspension under fasting conditions.
Administration of riluzole with food decreases AUC by 20% and peak plasma concentrations by 45%. Riluzole is 96% bound to plasma proteins, principally to albumin and lipoproteins. The drug is metabolized by cytochrome P-450 (CYP) 1A2 and by direct and sequential glucuronidation; some metabolites appear to be active in vitro, but the clinical importance is not known.
At least 88% of a dose is metabolized; 90% is excreted in urine (only 2% as unchanged drug) and 5% is excreted in feces. The half-life of riluzole is 12 hours.
USES: This medication is used to treat a certain type of nerve disease called amyotrophic lateral sclerosis (ALS, also commonly called Lou Gehrig's disease). Riluzole helps to slow down the worsening of this disease and prolong survival.
Generic name: riluzole
Pronunciation: (RIL-ue-zole)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Rilutek
Indications
The following indications are listed for Rilutek:
- Amyotrophic Lateral Sclerosis
Dosing
For the management of amyotrophic lateral sclerosis (ALS), the recommended dosage of riluzole is 50 mg twice daily. Higher daily dosages have not been shown to provide any additional benefit but may increase the risk of adverse effects.
Riluzole is administered orally twice daily (as tablets or oral suspension). Because food decreases oral bioavailability of the drug, the manufacturer recommends that riluzole be taken in a fasting state (e.g., 1 hour before or 2 hours after a meal).
Store riluzole tablets at 20-25degreesC and protect from bright light. Store the oral suspension upright at 20-25degreesC (excursions permitted to 15-30degreesC); protect from bright light and do not freeze. Use the oral suspension within 15 days of initially opening the bottle.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*History of severe hypersensitivity reactions to the drug or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects (>=5% and greater than placebo) with riluzole tablets include asthenia, nausea, dizziness, decreased lung function, and abdominal pain.
The most common adverse effects (>=5% and greater than placebo) with riluzole oral suspension include oral hypoesthesia, asthenia, nausea, decreased lung function, hypertension, and abdominal pain.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Efficacy and safety of riluzole have not been established in pediatric patients.
There are no adequate data to determine whether riluzole is associated with a risk of developmental abnormalities when used during pregnancy. In animal studies, administration of riluzole to pregnant rats and rabbits resulted in adverse developmental effects (e.g., decreased embryofetal/offspring viability, growth, and functional development) at clinically relevant doses.
If riluzole is used during pregnancy, the patient should be advised of the potential risk to the fetus.
It is not known whether riluzole is distributed into human milk. Riluzole or its metabolites have been detected in milk of lactating rats.
Patients should be advised that the potential for serious adverse effects in nursing infants from riluzole is not known.
The manufacturer does not recommend specific dosage adjustments in geriatric patients.
No overall differences in safety and efficacy have been observed in geriatric patients 65 years of age or older compared with younger adults. Age does not appear to have a clinically important effect on the pharmacokinetics of riluzole. However, greater sensitivity in some older individuals cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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