Stalevo 50 Tablets
Overview
What is this medicine?
How to Use This Medicine
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food. Swallow the tablet whole - do not chew, break, or crush it.
If you take an iron supplement or a multivitamin that contains iron, consult your doctor or pharmacist about how to take it with this medication. Iron may reduce the absorption of this medication in your body.
Your diet can also affect how well your body absorbs this medication. Diets high in protein, fat, or calories, as well as acidic foods, may reduce absorption. Discuss your diet with your doctor, especially if you plan to make any changes.
Important Warnings
Do not stop taking this medication suddenly without consulting your doctor, as this may increase your risk of side effects. If you need to stop taking this medication, your doctor will instruct you on how to taper off gradually.
Continue taking this medication even when you are not experiencing symptoms. Keeping a diary of your symptoms can be helpful in tracking your progress.
Dosage and Administration
Take this medication at the same time every day, as directed by your doctor or healthcare provider. Continue taking it even if you feel well.
Storage and Disposal
Store this medication at room temperature in a dry place, away from the bathroom. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly - do not flush them down the toilet or pour them down the drain unless instructed to do so. Consult your pharmacist if you have questions about the best way to dispose of medications. You may also want to check if there are any drug take-back programs in your area.
Missed Doses
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses.
Lifestyle & Tips
- Take Stalevo exactly as prescribed by your doctor. Do not stop taking it suddenly without consulting your doctor, as this can lead to serious side effects.
- You can take Stalevo with or without food. However, if you experience nausea, taking it with a low-protein snack may help. Avoid high-protein meals, as they can reduce the absorption of levodopa.
- Do not crush or chew the tablets; swallow them whole.
- Be aware that your urine, sweat, or saliva may turn a brownish-orange color. This is a harmless effect of entacapone.
- Stand up slowly from a sitting or lying position to minimize dizziness or lightheadedness (orthostatic hypotension).
- Report any new or worsening involuntary movements (dyskinesia), hallucinations, confusion, or unusual urges (like gambling or excessive shopping) to your doctor immediately.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Condition-Specific Dosing:
Pediatric Dosing
Dose Adjustments
Renal Impairment:
Hepatic Impairment:
Pharmacology
Mechanism of Action
Pharmacokinetics
Absorption:
Distribution:
Elimination:
Pharmacodynamics
Safety & Warnings
Side Effects
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
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
New or worsening behavioral or mood changes, including:
+ Depression
+ Thoughts of suicide
Hallucinations (seeing or hearing things that are not there)
Severe dizziness or fainting
Confusion
Vomiting blood or coffee ground-like material
Black, tarry, or bloody stools
Muscle pain or weakness, dark urine, or difficulty urinating
A new skin lump or growth
Changes in the color or size of a mole
Strong, uncontrollable urges (such as eating, gambling, sex, or spending money)
New or worsening trouble controlling body movements
Chest pain or pressure
Shortness of breath
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling extremely tired or weak
Sudden, unexplained sleepiness, especially during activities like driving, eating, or talking
If you experience sudden sleepiness, do not drive or engage in activities that require alertness while taking this medication. Inform your doctor immediately if you experience excessive sleepiness or fall asleep during activities.
Neuroleptic Malignant Syndrome (NMS)
NMS is a rare but potentially life-threatening condition that can occur when this medication is stopped abruptly or when the dose is lowered. If you experience any of the following symptoms, contact your doctor right away:
Fever
Muscle cramps or stiffness
Dizziness
Severe headache
Confusion
Changes in thinking
Rapid heartbeat
Abnormal heartbeat
Excessive sweating
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you experience any of the following side effects, contact your doctor if they bother you or do not resolve on their own:
Dizziness
Drowsiness
Fatigue
Weakness
Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Dry mouth
Headache
Trouble sleeping
Back pain
This is not an exhaustive list of possible side effects. If you have 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:
- Severe, persistent diarrhea (can be delayed onset and may indicate colitis)
- Unexplained muscle stiffness, high fever, confusion, sweating, or rapid heart rate (signs of Neuroleptic Malignant Syndrome-like reaction)
- New or worsening involuntary movements (dyskinesia)
- Hallucinations or delusions
- Excessive daytime sleepiness or sudden onset of sleep
- Unusual urges or behaviors (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating)
- Severe dizziness or fainting spells
- Yellowing of skin or eyes (jaundice), dark urine, or persistent nausea/vomiting (signs of liver problems)
Before Using This Medicine
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.
Certain health conditions, including:
+ Glaucoma
+ Skin lumps or growths
+ A history of skin cancer
If you have taken specific antidepressant medications, such as isocarboxazid, phenelzine, or tranylcypromine, within the last 14 days. Taking this medication too soon after these drugs can lead to severe high blood pressure.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor. Please provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products
Vitamins
* Any health problems you have
Your doctor will help you determine whether it is safe to take this medication with your other medications and health conditions. Do not start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
Until you know how this medication affects you, avoid driving and other activities that require alertness. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying position, and be cautious when climbing stairs.
Regular blood tests and other laboratory evaluations are crucial while taking this medication. Follow your doctor's instructions for scheduling these tests. Additionally, inform all your healthcare providers and laboratory personnel that you are taking this medication, as it may interfere with certain lab tests.
You may experience a decrease in the medication's effect as the time approaches for your next dose. If this occurs and bothers you, discuss it with your doctor. It may take several months to achieve the full therapeutic effect of this medication.
Before consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter medications that may cause drowsiness, consult with your doctor.
You may notice a dark discoloration (red, brown, or black) in your saliva, urine, or sweat while taking this medication. Although this is harmless, it may stain your clothing.
If you experience diarrhea or vomiting, consult your doctor promptly. It is crucial to prevent dehydration and electrolyte imbalances.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to you and your baby.
Overdose Information
Overdose Symptoms:
- Severe dyskinesia
- Agitation
- Confusion
- Orthostatic hypotension
- Nausea and vomiting
- Tachycardia
- Arrhythmias
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment is supportive, including gastric lavage, activated charcoal, and careful monitoring of vital signs and cardiac rhythm.
Drug Interactions
Contraindicated Interactions
- Non-selective monoamine oxidase (MAO) inhibitors (e.g., phenelzine, tranylcypromine) - risk of hypertensive crisis. Must be discontinued at least 2 weeks prior to Stalevo initiation.
Major Interactions
- MAO-A inhibitors (e.g., moclobemide) - risk of hypertensive crisis.
- Iron salts (ferrous sulfate, gluconate) - form chelates with entacapone, reducing absorption of both. Administer Stalevo at least 2-3 hours before or after iron preparations.
- Dopamine D2 receptor antagonists (e.g., antipsychotics like haloperidol, chlorpromazine; antiemetics like metoclopramide) - may antagonize the effects of levodopa and worsen Parkinson's symptoms.
- Pyridoxine (Vitamin B6) - can reverse the effects of levodopa if not combined with carbidopa; however, Stalevo contains carbidopa, mitigating this interaction.
Moderate Interactions
- Antihypertensive agents - additive hypotensive effects, especially orthostatic hypotension.
- Tricyclic antidepressants (TCAs) - potential for hypertension and dyskinesia, though generally safe with carbidopa/levodopa.
- CNS depressants (e.g., sedatives, hypnotics, opioids) - additive sedative effects.
- Sympathomimetics (e.g., epinephrine, norepinephrine, dopamine, dobutamine, isoproterenol) - entacapone may potentiate their effects due to COMT inhibition, increasing risk of arrhythmias and hypertension. Use with caution.
Minor Interactions
- Protein-rich foods - may reduce levodopa absorption.
Monitoring
Baseline Monitoring
Rationale: Entacapone is metabolized by the liver; baseline assessment is important, especially in patients with pre-existing hepatic impairment.
Timing: Prior to initiation of therapy.
Rationale: To assess baseline kidney function, as entacapone metabolites are renally excreted.
Timing: Prior to initiation of therapy.
Rationale: To assess for baseline orthostatic hypotension, a common side effect of dopaminergic therapy.
Timing: Prior to initiation of therapy.
Rationale: To establish baseline hematologic parameters.
Timing: Prior to initiation of therapy.
Routine Monitoring
Frequency: Regularly at follow-up visits (e.g., every 1-3 months initially, then every 3-6 months)
Target: Optimal control of Parkinson's symptoms with minimal dyskinesia and 'off' time.
Action Threshold: Worsening dyskinesia or increased 'off' time may require dose adjustment or addition of other therapies.
Frequency: Regularly at follow-up visits (e.g., every 1-3 months initially, then every 3-6 months)
Target: Maintain within patient's normal range, minimize orthostatic drop.
Action Threshold: Significant orthostatic hypotension (e.g., >20 mmHg systolic or >10 mmHg diastolic drop) may require dose adjustment or intervention.
Frequency: Regularly at follow-up visits (e.g., every 1-3 months initially, then every 3-6 months)
Target: Maintain cognitive function and absence of problematic behavioral changes.
Action Threshold: New onset or worsening of these symptoms requires prompt evaluation and potential dose adjustment or discontinuation.
Frequency: Periodically, especially if symptoms of liver dysfunction develop or if patient has pre-existing hepatic impairment.
Target: Within normal limits.
Action Threshold: Significant elevation (e.g., >3x ULN) may warrant dose reduction or discontinuation.
Symptom Monitoring
- Dyskinesia (involuntary movements)
- Nausea/Vomiting
- Orthostatic hypotension (dizziness upon standing)
- Hallucinations
- Confusion
- Sleep disturbances (insomnia, somnolence, sudden sleep onset)
- Impulse control disorders (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating)
- Diarrhea (can be severe and delayed onset)
- Urine discoloration (brownish-orange, harmless)
- Muscle stiffness, fever, confusion (Neuroleptic Malignant Syndrome-like symptoms, especially upon abrupt withdrawal)
Special Patient Groups
Pregnancy
Category C. Stalevo should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects.
Trimester-Specific Risks:
Lactation
Levodopa is excreted into human breast milk and may inhibit lactation. Entacapone and carbidopa are also likely excreted. Due to 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.
Pediatric Use
The safety and effectiveness of Stalevo in pediatric patients have not been established. Use is not recommended.
Geriatric Use
No specific dose adjustment is generally required based on age alone. However, elderly patients may be more sensitive to the central nervous system and cardiovascular side effects (e.g., orthostatic hypotension, hallucinations, confusion) and should be monitored closely. Start with lower doses and titrate carefully.
Clinical Information
Clinical Pearls
- Stalevo is specifically indicated for patients with Parkinson's disease who are experiencing 'wearing-off' phenomena on their current levodopa/carbidopa regimen.
- Patients should be advised about the harmless brownish-orange discoloration of urine, sweat, and saliva that can occur with entacapone.
- Severe, sometimes delayed-onset, diarrhea can occur with entacapone. Patients should be instructed to report persistent diarrhea, as it may indicate entacapone-induced colitis.
- Abrupt discontinuation or rapid dose reduction of Stalevo can lead to a symptom complex resembling Neuroleptic Malignant Syndrome (NMS), including fever, muscle rigidity, altered mental status, and autonomic instability. Taper slowly if discontinuation is necessary.
- Monitor for impulse control disorders (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating), which can occur with dopaminergic therapies. Patients and caregivers should be educated about these potential side effects.
- Iron supplements should be taken at least 2-3 hours apart from Stalevo to avoid reduced absorption of both medications.
Alternative Therapies
- Dopamine Agonists (e.g., pramipexole, ropinirole, rotigotine)
- MAO-B Inhibitors (e.g., rasagiline, selegiline, safinamide)
- Other COMT Inhibitors (e.g., opicapone, tolcapone - note: tolcapone has liver toxicity risk and requires LFT monitoring)
- Amantadine (for dyskinesia and motor fluctuations)
- Istradefylline (adenosine A2A receptor antagonist, for 'off' episodes)