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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| 5 mg/mL | LIQUID | ORAL | 70726-0304 |
| 5 mg/mL | LIQUID | ORAL | 70726-0306 |
| 5 mg/mL | LIQUID | ORAL | 70726-0305 |
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Teglutik, you must consult a qualified healthcare professional.
Detailed information about Teglutik
Riluzole is a benzothiazole derivative and glutamate antagonist indicated for the treatment of amyotrophic lateral sclerosis (ALS). It is designed to extend survival or delay the need for mechanical ventilation by modulating excitatory neurotransmission.
The standard, FDA-recommended dosage for Riluzole in adults with Amyotrophic Lateral Sclerosis (ALS) is 50 mg taken orally every 12 hours. This results in a total daily dose of 100 mg. Clinical data have shown that increasing the dose beyond 100 mg per day does not provide additional therapeutic benefit but does significantly increase the risk of adverse effects, particularly liver enzyme elevations and gastrointestinal distress.
Consistency is vital when taking Riluzole. Patients are encouraged to take their doses at the same time each day (e.g., 8:00 AM and 8:00 PM) to maintain steady levels of the medication in the bloodstream.
Riluzole is not approved for use in pediatric patients. The safety and effectiveness of Riluzole in children and adolescents under the age of 18 have not been established. ALS is an adult-onset disease, and the pharmacological profile of Riluzole in developing biological systems is unknown. If a child accidentally ingests Riluzole, seek emergency medical attention immediately.
Specific dosage adjustment guidelines for patients with renal (kidney) impairment are not well-defined. However, since the drug is primarily metabolized by the liver, mild to moderate renal impairment may not require a dose change. In cases of severe renal impairment, healthcare providers will exercise extreme caution and monitor the patient closely for signs of toxicity.
Riluzole is contraindicated (should not be used) in patients with baseline serum transaminases (ALT/AST) greater than 3 times the upper limit of normal (ULN). For patients with mild hepatic impairment, the drug should be used with significant caution. Because the liver is the primary site of Riluzole metabolism, any decrease in liver function can lead to dangerously high levels of the drug in the body.
No specific dosage adjustments are generally required for geriatric patients based solely on age. However, because elderly patients are more likely to have decreased hepatic or renal function and may be taking multiple other medications, doctors typically start with the standard dose but monitor the patient more frequently for side effects.
To ensure the best possible absorption and efficacy, follow these specific administration instructions:
If you miss a dose of Riluzole, skip the missed dose and take your next dose at the regularly scheduled time. Do not take two doses at once to make up for a missed one. Taking a double dose can increase the risk of serious side effects, such as extreme dizziness or liver toxicity.
Signs of a Riluzole overdose may include severe encephalopathy (brain dysfunction), extreme drowsiness, agitation, or even coma. In some cases, methemoglobinemia (a blood disorder where oxygen cannot be effectively released to tissues) has been reported.
In the event of a suspected overdose, contact your local poison control center or seek emergency medical care immediately. There is no specific antidote for Riluzole; treatment is supportive and focused on managing symptoms.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking the medication without medical guidance, as this could impact the effectiveness of your treatment plan.
Like all medications, Riluzole can cause side effects, although not everyone experiences them. The most frequently reported adverse reactions include:
Riluzole is a potent medication that requires careful medical supervision. It is specifically designed for Amyotrophic Lateral Sclerosis (ALS) and should not be used for other conditions without specialist consultation. The most critical safety aspect of Riluzole therapy is the risk of liver injury, which can be asymptomatic (showing no symptoms) in its early stages. Therefore, adherence to laboratory monitoring schedules is mandatory for all patients.
There are currently no FDA black box warnings for Riluzole. However, the FDA-approved labeling contains significant warnings regarding hepatotoxicity (liver damage) and neutropenia (low white blood cell count).
Clinical trials have shown that Riluzole can cause elevations in serum transaminases (liver enzymes). In most cases, these elevations occur within the first 3 months of treatment. While many cases are mild, severe liver injury and even fatalities have been reported. If ALT levels rise to 5 times the upper limit of normal, the drug must be discontinued immediately.
There are few absolute contraindications for drug combinations with Riluzole, but substances that cause severe liver toxicity should be avoided.
Since Riluzole is metabolized by the CYP1A2 enzyme, any drug that inhibits this enzyme will cause Riluzole levels to rise, increasing the risk of toxicity. Examples include:
There are specific circumstances under which Riluzole must NEVER be used because the risks clearly outweigh any potential benefits:
Riluzole is classified by the FDA as Pregnancy Category C (under the older system). This means that studies in animals have shown adverse effects on the fetus (such as decreased fertility and increased embryolethality), but there are no adequate and well-controlled studies in humans. It is not known whether Riluzole can cause fetal harm when administered to a pregnant woman. Consequently, Riluzole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Women of childbearing age should discuss contraception with their doctor while taking this medication.
It is not known if Riluzole is excreted in human milk. Many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants (including liver toxicity and neurological effects), a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. Most clinical guidelines recommend against breastfeeding while taking Riluzole.
Riluzole is a glutamate modulator. Its primary therapeutic action in ALS is thought to be the inhibition of glutamate release from presynaptic terminals. It achieves this by blocking voltage-gated sodium channels (specifically the Nav1.6 subtype), which prevents the repetitive firing of action potentials that lead to neurotransmitter release. Additionally, Riluzole may increase the clearance of glutamate from the synapse by enhancing the activity of excitatory amino acid transporters (EAATs) on astrocytes. By reducing the overall 'glutamatergic tone,' Riluzole protects motor neurons from calcium-mediated apoptosis (programmed cell death) caused by excitotoxicity.
Common questions about Teglutik
Riluzole is primarily used to treat Amyotrophic Lateral Sclerosis (ALS), also known as Lou Gehrig's disease. It is a neuroprotective medication that works by modulating the neurotransmitter glutamate, which is often found in excessive levels in ALS patients. By reducing glutamate-induced damage to motor neurons, Riluzole can extend the life of a patient or delay the need for a tracheostomy. It is important to note that Riluzole does not cure ALS or reverse existing muscle weakness. It is typically used as part of a comprehensive treatment plan to slow disease progression. Your doctor will determine if it is appropriate based on your specific diagnosis and liver health.
The most common side effects associated with Riluzole include nausea, dizziness, stomach pain, and a general feeling of weakness or fatigue (asthenia). Many patients also report a tingling sensation around the mouth, known as circumoral paresthesia. Some individuals may experience a decrease in lung function or an increase in liver enzymes, which requires regular blood monitoring. Most of the gastrointestinal side effects occur early in treatment and may improve over time. However, if you experience severe vomiting or signs of liver trouble like yellowing of the skin, contact your doctor immediately. Always report any new or worsening symptoms to your healthcare team during your regular checkups.
It is strongly recommended that you avoid or significantly limit alcohol consumption while taking Riluzole. Both Riluzole and alcohol are processed by the liver and can cause hepatic stress. Combining the two greatly increases the risk of developing severe liver damage or hepatotoxicity. Furthermore, alcohol can enhance the side effects of Riluzole, such as dizziness and drowsiness, which may increase the risk of falls and accidents. Since ALS patients may already struggle with balance and coordination, this combination can be particularly dangerous. Discuss your alcohol intake honestly with your doctor before starting this medication to ensure your safety.
The safety of Riluzole during pregnancy has not been established in human clinical trials. Animal studies have indicated that the drug may cause harm to a developing fetus, leading to its classification as a Pregnancy Category C medication. Because of these potential risks, Riluzole is generally not recommended for use during pregnancy unless the benefits to the mother clearly outweigh the risks to the baby. Women who are pregnant or planning to become pregnant should have a detailed discussion with their neurologist about the risks and benefits. It is also unknown if the drug passes into breast milk, so breastfeeding is typically discouraged while on Riluzole. Your healthcare provider can help you navigate these complex decisions.
Riluzole does not provide immediate relief of symptoms, and patients will not 'feel' the drug working in the way they might feel a painkiller. Its benefits are neuroprotective and occur at the cellular level over a long period. In clinical trials, the difference in survival and disease progression between patients taking Riluzole and those taking a placebo only became statistically significant after several months of treatment. It is designed to slow the progression of ALS rather than stop it or reverse it. Therefore, it is crucial to take the medication consistently as prescribed, even if you do not notice an immediate change in your physical abilities. Your doctor will monitor your progress through regular clinical assessments.
While Riluzole does not cause a traditional withdrawal syndrome or physical dependence, you should never stop taking it suddenly without consulting your neurologist. Stopping the medication will end the neuroprotective effects it provides, which could potentially allow the symptoms of ALS to progress at a faster rate. If you are experiencing side effects that make you want to stop the drug, your doctor may be able to offer solutions, such as switching to a liquid formulation or adjusting the timing of your doses. Always have a plan with your healthcare provider before making any changes to your medication regimen. They will help you weigh the benefits of continued treatment against any discomfort you may be experiencing.
If you miss a dose of Riluzole, you should skip the missed dose entirely and take your next dose at the regularly scheduled time. Do not attempt to 'double up' or take two doses at once to compensate for the one you missed. Taking too much Riluzole at one time can significantly increase the risk of serious side effects, including liver enzyme spikes and severe dizziness. To help you remember your doses, it may be useful to use a pill organizer or set an alarm on your phone. Consistency is key to maintaining the correct level of medication in your system. If you miss several doses in a row, contact your doctor's office for further instructions.
Weight gain is not a typical side effect of Riluzole. In fact, many patients with ALS struggle with weight loss due to muscle atrophy and difficulty swallowing (dysphagia). Riluzole is more commonly associated with nausea and a decrease in appetite, which could potentially lead to weight loss in some individuals. If you notice significant changes in your weight while taking Riluzole, it is important to discuss this with your healthcare team. They can determine if the change is related to the medication, your diet, or the progression of the ALS itself. Nutritional support is a vital part of ALS care, and your doctor may recommend a consultation with a dietitian.
Riluzole can interact with several other medications, particularly those that affect the liver or are processed by the same liver enzymes (CYP1A2). For example, certain antibiotics like ciprofloxacin or antidepressants like fluvoxamine can increase Riluzole levels in your blood, raising the risk of toxicity. On the other hand, smoking or taking certain other drugs can make Riluzole less effective. It is also important to be cautious with over-the-counter medicines like acetaminophen (Tylenol) that can affect the liver. Always provide your doctor and pharmacist with a complete list of all medications, supplements, and herbal products you are using. They will check for potential interactions and adjust your treatment plan accordingly to ensure your safety.
Yes, Riluzole is available as a generic medication in the form of 50 mg oral tablets. Generic versions are typically more cost-effective than the brand-name version, Rilutek, while providing the same active ingredient and therapeutic effect. However, some of the newer formulations, such as the oral suspension (Tiglutik) or the oral film (Exservan), may still be under patent protection and might not have generic equivalents available yet. If cost is a concern, you should speak with your pharmacist or insurance provider to see if a generic version is covered under your plan. Your doctor can also help determine which formulation is most appropriate for your specific needs and swallowing ability.
Other drugs with the same active ingredient (Riluzole)
These side effects occur in a smaller percentage of patients but are still well-documented:
> Warning: Stop taking Riluzole and call your doctor immediately if you experience any of the following serious symptoms:
The primary concern with long-term Riluzole use is the cumulative effect on the liver. Because ALS is a chronic condition, patients may be on Riluzole for years. Continuous monitoring of liver function is required for the duration of therapy. There is no evidence that Riluzole causes long-term cognitive impairment or permanent damage to other organ systems, provided that liver and lung health are monitored.
No FDA black box warnings currently exist for Riluzole. However, the warnings regarding liver toxicity are considered 'major' and are featured prominently in the 'Warnings and Precautions' section of the prescribing information. The FDA requires that liver function tests be performed before starting the drug and at regular intervals thereafter.
Report any unusual symptoms or changes in your health to your healthcare provider promptly. Keeping a 'symptom diary' can be helpful for your doctor to determine if a side effect is related to the medication or the progression of ALS.
Cases of ILD have been reported in patients treated with Riluzole. If respiratory symptoms develop (such as a dry cough or difficulty breathing), the drug should be stopped until a lung evaluation is performed. If ILD is confirmed, Riluzole must be permanently discontinued.
Patients should be alert for any signs of infection (fever, sore throat). Riluzole can cause a drop in white blood cell counts (neutropenia), which weakens the immune system. If a low white blood cell count is detected, the medication may need to be stopped.
Because Riluzole can cause somnolence (drowsiness) and dizziness, patients should be cautious when performing tasks that require mental alertness.
To ensure safety, healthcare providers will require the following tests:
Riluzole may cause dizziness or sleepiness. Do not drive, operate heavy machinery, or engage in dangerous activities until you know how Riluzole affects you. If you feel drowsy or lightheaded, avoid these tasks and consult your doctor.
Avoid or strictly limit alcohol consumption while taking Riluzole. Alcohol is a known hepatotoxin (liver-damaging substance). Combining alcohol with Riluzole significantly increases the risk of severe liver damage. Additionally, alcohol can worsen the dizziness and drowsiness caused by the medication.
There is no evidence of a 'withdrawal syndrome' associated with Riluzole. However, you should not stop taking the medication without discussing it with your neurologist. Stopping the drug will end its neuroprotective benefits, which may lead to a faster progression of ALS symptoms toward respiratory failure.
> Important: Discuss all your medical conditions, especially any history of liver or kidney disease, with your healthcare provider before starting Riluzole. Be sure to mention if you are a smoker, as tobacco use can decrease the effectiveness of the drug.
Conversely, drugs or substances that induce (speed up) the CYP1A2 enzyme will cause Riluzole to be cleared from the body too quickly, reducing its effectiveness. Examples include:
Riluzole does not typically interfere with standard laboratory test results (like glucose or cholesterol tests), but it will directly cause changes in Liver Function Tests (ALT/AST). It is important that the laboratory and your doctors know you are taking Riluzole when they interpret these specific results.
If you must take a medication that interacts with Riluzole, your doctor may:
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking. This includes over-the-counter pain relievers like acetaminophen (Tylenol), which also affects the liver.
These are conditions where Riluzole might be used, but only with extreme caution and frequent monitoring:
There is no well-documented cross-sensitivity between Riluzole and other major drug classes. However, patients who are sensitive to other benzothiazole derivatives (used in some industrial processes or other rare medications) should inform their doctor.
Always provide a full medical history to your neurologist, including any history of hepatitis, heavy alcohol use, or previous drug allergies.
> Important: Your healthcare provider will evaluate your complete medical history, including liver health and current medications, before determining if Riluzole is safe for you.
Clinical studies of Riluzole included a significant number of patients aged 65 and over. No overall differences in safety or effectiveness were observed between these older patients and younger patients. However, the elderly are generally more likely to have decreased hepatic, renal, or cardiac function.
The pharmacokinetics of Riluzole have not been extensively studied in patients with renal failure. However, about 90% of a Riluzole dose is recovered in the urine as metabolites. While the parent drug is metabolized by the liver, the accumulation of metabolites in patients with severe renal impairment (CrCl < 30 mL/min) could potentially lead to unforeseen side effects. Use in this population requires clinical vigilance.
This is the most critical special population for Riluzole.
> Important: Special populations require individualized medical assessment. Always inform your healthcare team about your age, pregnancy status, and any organ-specific health issues.
| Parameter | Value |
|---|---|
| Bioavailability | ~60% (decreased by high-fat food) |
| Protein Binding | ~96% (primarily Albumin) |
| Half-life | ~12 hours |
| Tmax | 1.0 to 1.5 hours |
| Metabolism | Hepatic (Primary: CYP1A2; Secondary: CYP2D6) |
| Excretion | Renal (90% as metabolites), Fecal (5%) |
Riluzole is the prototypical member of the benzothiazole class of glutamate antagonists. While other drugs target glutamate receptors (like Memantine for Alzheimer's), Riluzole is unique in its focus on inhibiting glutamate release and its specific application in motor neuron disease. It is often categorized as a 'neuroprotective agent' or 'antiglutamatergic.'