Nourianz 40mg Tablets
It is used to treat Parkinson's disease.
Drug Class
Antiparkinsonian agent
Pharmacologic Class
Adenosine A2A receptor antagonist
Pregnancy Category
Not available
FDA Approved
Aug 2019
DEA Schedule
Not Controlled
Overview
What is this medicine?
Nourianz is a medication used along with other Parkinson's disease medicines (like levodopa) to help reduce the amount of 'off' time, which is when your Parkinson's symptoms return or worsen between doses of your other medications. It works by targeting specific receptors in the brain.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all accompanying information carefully. You can take this medication with or without food. It's essential to continue taking this medication as directed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry location, avoiding the bathroom. Keep all medications in a secure place, out of reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult your pharmacist for guidance on proper disposal. You may also want to explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To use this medication correctly, follow your doctor's instructions and read all accompanying information carefully. You can take this medication with or without food. It's essential to continue taking this medication as directed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry location, avoiding the bathroom. Keep all medications in a secure place, out of reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult your pharmacist for guidance on proper disposal. You may also want to explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take Nourianz exactly as prescribed by your doctor, usually once a day.
- It can be taken with or without food.
- Do not crush, chew, or break the tablet.
- Do not stop taking Nourianz suddenly without talking to your doctor.
- Report any new or worsening uncontrolled movements (dyskinesia) to your doctor.
- Be aware of potential changes in behavior, such as hallucinations, delusions, or unusual urges (e.g., gambling, shopping, eating). Report these to your doctor immediately.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
20 mg orally once daily, may increase to 40 mg orally once daily based on efficacy and tolerability.
Dose Range:
20 - 40 mg
Condition-Specific Dosing:
concomitant strong CYP3A4 inhibitors:
Reduce dose to 20 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed.
Moderate:
No dose adjustment needed.
Severe:
No dose adjustment needed (eGFR < 30 mL/min/1.73 m^2).
Dialysis:
Not studied in patients with end-stage renal disease (ESRD) requiring dialysis. Use with caution.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh A).
Moderate:
Maximum dose of 20 mg once daily (Child-Pugh B).
Severe:
Not recommended (Child-Pugh C).
Pharmacology
Mechanism of Action
Istradefylline is a selective adenosine A2A receptor antagonist. The exact mechanism of action in Parkinson's disease is unknown, but it is thought to involve antagonism of adenosine A2A receptors in the basal ganglia, which are involved in regulating motor function. By blocking these receptors, istradefylline may help to reduce 'off' time in patients with Parkinson's disease.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 94%
Tmax:
1-2 hours
FoodEffect:
No clinically significant effect of food on absorption.
Distribution:
Vd:
Approximately 1000 L
ProteinBinding:
Approximately 99%
CnssPenetration:
Yes
Elimination:
HalfLife:
Approximately 18 hours
Clearance:
Approximately 30 L/hour
ExcretionRoute:
Urine (approximately 70%), Feces (approximately 30%)
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Not precisely defined for clinical effect, but pharmacokinetic onset is rapid.
PeakEffect:
Not precisely defined for clinical effect, but pharmacokinetic peak is 1-2 hours.
DurationOfAction:
Approximately 24 hours (consistent with once-daily dosing).
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
New or worsening trouble controlling body movements
New or worsening mental, mood, or behavior changes
Hallucinations (seeing or hearing things that are not there)
Feeling confused
Strong, uncontrollable urges (such as eating, gambling, sex, or spending money)
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Dizziness
Constipation
Upset stomach
Trouble sleeping
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
New or worsening trouble controlling body movements
New or worsening mental, mood, or behavior changes
Hallucinations (seeing or hearing things that are not there)
Feeling confused
Strong, uncontrollable urges (such as eating, gambling, sex, or spending money)
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Dizziness
Constipation
Upset stomach
Trouble sleeping
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- New or worsening uncontrolled movements (dyskinesia)
- Seeing or hearing things that are not real (hallucinations)
- Unusual thoughts or behaviors (e.g., paranoia, delusions)
- Strong urges that are difficult to control (e.g., gambling, shopping, eating, sexual urges)
- Difficulty sleeping (insomnia)
- Dizziness or lightheadedness
- Nausea
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
A history of mental health or behavioral problems, as these may be relevant to your treatment.
Existing liver disease, as this may affect how your body processes the medication.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial because certain medications, such as those used to treat HIV, infections, seizures, and other conditions, may interact with this drug and should not be taken concurrently.
Please note that this is not an exhaustive list of all potential drug interactions or health problems that may be relevant to your treatment. To ensure your safety, it is vital to:
Inform your doctor and pharmacist about all your medications (prescription and OTC), natural products, vitamins, and health problems.
Verify that it is safe to take this medication with all your other medications and health conditions.
* Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
A history of mental health or behavioral problems, as these may be relevant to your treatment.
Existing liver disease, as this may affect how your body processes the medication.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial because certain medications, such as those used to treat HIV, infections, seizures, and other conditions, may interact with this drug and should not be taken concurrently.
Please note that this is not an exhaustive list of all potential drug interactions or health problems that may be relevant to your treatment. To ensure your safety, it is vital to:
Inform your doctor and pharmacist about all your medications (prescription and OTC), natural products, vitamins, and health problems.
Verify that it is safe to take this medication with all your other medications and health conditions.
* Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you smoke or use any other tobacco products, discuss this with your doctor, as your dosage may need to be adjusted if you start or stop smoking or using these products.
This medication can pose a risk to an unborn baby. If there is a chance you may become pregnant, it is crucial to use effective birth control while taking this drug. If you do become pregnant, notify your doctor immediately. Additionally, if you are breastfeeding, consult with your doctor to discuss any potential risks to your baby and determine the best course of action.
This medication can pose a risk to an unborn baby. If there is a chance you may become pregnant, it is crucial to use effective birth control while taking this drug. If you do become pregnant, notify your doctor immediately. Additionally, if you are breastfeeding, consult with your doctor to discuss any potential risks to your baby and determine the best course of action.
Overdose Information
Overdose Symptoms:
- Exacerbation of known adverse reactions (e.g., dyskinesia, hallucinations, insomnia, dizziness, nausea).
What to Do:
There is no specific antidote for istradefylline overdose. Treatment should be symptomatic and supportive. Contact a poison control center immediately (e.g., 1-800-222-1222) or seek emergency medical attention.
Drug Interactions
Major Interactions
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort): Avoid coadministration due to significant decrease in istradefylline exposure.
Moderate Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir): Reduce istradefylline dose to 20 mg once daily.
- Smoking (CYP1A2 inducer): May decrease istradefylline exposure; consider dose adjustment if smoking status changes.
Monitoring
Baseline Monitoring
Assessment of motor fluctuations ('off' time)
Rationale: To establish baseline severity of Parkinson's disease symptoms and motor complications.
Timing: Prior to initiation of therapy.
Psychiatric history (e.g., psychosis, impulse control disorders)
Rationale: To identify predisposition to psychiatric adverse events.
Timing: Prior to initiation of therapy.
Routine Monitoring
Dyskinesia
Frequency: Regularly, especially after dose adjustments or initiation.
Target: Minimize severity and frequency.
Action Threshold: If new or worsening dyskinesia occurs, consider reducing the dose of istradefylline or concomitant dopaminergic medications (e.g., levodopa).
Psychiatric symptoms (e.g., hallucinations, delusions, psychotic behavior, impulse control disorders)
Frequency: Regularly, especially after dose adjustments or initiation.
Target: Absence of new or worsening symptoms.
Action Threshold: If new or worsening psychiatric symptoms occur, consider dose reduction or discontinuation of istradefylline.
Symptom Monitoring
- New or worsening dyskinesia
- Hallucinations
- Delusions
- Psychotic behavior
- Impulse control disorders (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating)
- Insomnia
- Dizziness
- Nausea
Special Patient Groups
Pregnancy
There are no adequate data on the developmental risk associated with the use of istradefylline in pregnant women. Animal studies showed adverse developmental effects at exposures higher than clinical. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Limited human data. Animal studies suggest potential for developmental toxicity at high doses.
Second Trimester:
Limited human data. Animal studies suggest potential for developmental toxicity at high doses.
Third Trimester:
Limited human data. Animal studies suggest potential for developmental toxicity at high doses.
Lactation
It is unknown if istradefylline is excreted in human milk. Animal studies showed excretion into milk. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Moderate risk (L3) - No human data, but animal data suggest excretion into milk. Potential for adverse effects on the infant.
Pediatric Use
The safety and effectiveness of Nourianz in pediatric patients have not been established. It is not indicated for use in this population.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger adult patients in clinical trials. No specific dose adjustment is required based on age alone, but elderly patients may be more sensitive to adverse effects, particularly psychiatric symptoms and dyskinesia. Monitor closely.
Clinical Information
Clinical Pearls
- Nourianz is an adjunctive therapy to levodopa/carbidopa for Parkinson's disease patients experiencing 'off' episodes.
- It is not indicated as monotherapy for Parkinson's disease.
- The most common adverse reaction is dyskinesia, which may require dose adjustment of either Nourianz or concomitant dopaminergic medications.
- Patients should be monitored for psychiatric adverse reactions, including hallucinations, delusions, and impulse control disorders.
- Avoid coadministration with strong CYP3A4 inducers. Reduce dose with strong CYP3A4 inhibitors.
- Consider the patient's smoking status, as smoking can reduce istradefylline exposure.
Alternative Therapies
- COMT inhibitors (e.g., entacapone, opicapone, tolcapone)
- MAO-B inhibitors (e.g., rasagiline, selegiline, safinamide)
- Dopamine agonists (e.g., pramipexole, ropinirole, rotigotine, apomorphine)
- Amantadine (for dyskinesia and 'off' time)
- Other adjunctive therapies for motor fluctuations (e.g., subcutaneous apomorphine, carbidopa/levodopa enteral suspension, inhaled levodopa)
Cost & Coverage
Average Cost:
Typically $1000 - $1500+ per 30 tablets
Insurance Coverage:
Specialty Tier (requires prior authorization, step therapy)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to consult with your pharmacist. If you have any questions or concerns about this medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount, and the time it occurred.