Stalevo 50 Tablets

Manufacturer ALMATICA Active Ingredient Levodopa, Carbidopa, and Entacapone(lee voe DOE pa, kar bi DOE pa, & en TA ka pone) Pronunciation LEE voe DOE pa, KAR bi DOE pa, & en TA ka pone
It is used to treat Parkinson's disease.
đŸˇī¸
Drug Class
Antiparkinsonian agents
đŸ§Ŧ
Pharmacologic Class
Dopamine precursor; DOPA decarboxylase inhibitor; Catechol-O-methyltransferase (COMT) inhibitor
🤰
Pregnancy Category
Category C
✅
FDA Approved
Mar 2003
âš–ī¸
DEA Schedule
Not Controlled

Overview

â„šī¸

What is this medicine?

Stalevo is a medication used to treat Parkinson's disease, especially when symptoms like stiffness, tremors, and difficulty moving return between doses of your regular Parkinson's medicine. It combines three ingredients: levodopa (which turns into dopamine in your brain), carbidopa (which helps more levodopa get to your brain), and entacapone (which helps levodopa last longer in your body). This combination helps to extend the 'on' time when your symptoms are well-controlled.
📋

How to Use This Medicine

Taking Your Medication

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.

Dosing & Administration

đŸ‘¨â€âš•ī¸

Adult Dosing

Standard Dose: Individualized based on levodopa requirements, typically one tablet of Stalevo 50 with each dose of levodopa/carbidopa, up to a maximum of 8 tablets per day (1600 mg entacapone).
Dose Range: 1 - 8 mg

Condition-Specific Dosing:

Parkinson's Disease with End-of-Dose Wearing-Off: Initiate with Stalevo 50 (50 mg levodopa, 12.5 mg carbidopa, 200 mg entacapone) if current levodopa/carbidopa dose is 50/12.5 mg. Adjust dose and frequency based on clinical response and tolerability, ensuring total daily entacapone does not exceed 1600 mg.
đŸ‘ļ

Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
âš•ī¸

Dose Adjustments

Renal Impairment:

Mild: No specific adjustment needed.
Moderate: No specific adjustment needed.
Severe: Use with caution; monitor for increased adverse effects (e.g., dyskinesia) due to potential accumulation of entacapone metabolites. Dose reduction may be considered.
Dialysis: Use with caution; monitor for increased adverse effects. Entacapone is highly protein bound and not significantly removed by dialysis.

Hepatic Impairment:

Mild: No specific adjustment needed.
Moderate: Use with caution; consider dose reduction, especially if signs of hepatic impairment are present. Monitor for adverse effects.
Severe: Use with caution; significant dose reduction may be necessary due to reduced entacapone clearance. Monitor closely for adverse effects.

Pharmacology

đŸ”Ŧ

Mechanism of Action

Levodopa, a precursor of dopamine, crosses the blood-brain barrier and is converted to dopamine in the brain. Carbidopa, a peripheral DOPA decarboxylase inhibitor, prevents the peripheral conversion of levodopa to dopamine, increasing the amount of levodopa available to the brain and reducing peripheral side effects. Entacapone, a reversible and selective catechol-O-methyltransferase (COMT) inhibitor, prevents the peripheral degradation of levodopa by COMT, thereby increasing the bioavailability and prolonging the plasma half-life of levodopa, leading to more sustained dopaminergic stimulation in the brain.
📊

Pharmacokinetics

Absorption:

Bioavailability: Levodopa: ~30% (variable); Carbidopa: ~58%; Entacapone: ~35%
Tmax: Levodopa: 1-2 hours; Carbidopa: 1-2 hours; Entacapone: 1-2 hours
FoodEffect: High-protein meals can significantly reduce the absorption of levodopa. Entacapone absorption is not significantly affected by food, but taking Stalevo with food may reduce GI upset.

Distribution:

Vd: Levodopa: ~0.9-1.6 L/kg; Carbidopa: ~1.1 L/kg; Entacapone: ~0.27 L/kg
ProteinBinding: Levodopa: 10-30%; Carbidopa: ~36%; Entacapone: >98% (primarily to albumin)
CnssPenetration: Levodopa: Yes; Carbidopa: Limited; Entacapone: Limited

Elimination:

HalfLife: Levodopa: ~1.5 hours (when co-administered with carbidopa and entacapone); Carbidopa: ~2 hours; Entacapone: ~2.4 hours
Clearance: Levodopa: Not readily quantifiable due to extensive metabolism; Carbidopa: Not readily quantifiable; Entacapone: ~0.7 L/min
ExcretionRoute: Levodopa: Urine (metabolites); Carbidopa: Urine (metabolites); Entacapone: Urine (10-20% as metabolites), Feces (80-90% as metabolites)
Unchanged: Levodopa: <1% (urine); Carbidopa: ~30% (urine); Entacapone: <0.2% (urine)
âąī¸

Pharmacodynamics

OnsetOfAction: Variable, typically within 30-60 minutes for levodopa effect
PeakEffect: 1-2 hours
DurationOfAction: Extended compared to levodopa/carbidopa alone, typically 2-4 hours per dose, depending on individual patient response and disease severity.

Safety & Warnings

âš ī¸

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
+ 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

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.
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.
âš ī¸

Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This will help ensure they have a complete understanding of your treatment plan.

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

đŸšĢ

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.
đŸŸĸ

Minor Interactions

  • Protein-rich foods - may reduce levodopa absorption.

Monitoring

đŸ”Ŧ

Baseline Monitoring

Liver Function Tests (LFTs)

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.

Renal Function (BUN, Creatinine)

Rationale: To assess baseline kidney function, as entacapone metabolites are renally excreted.

Timing: Prior to initiation of therapy.

Blood Pressure (sitting and standing)

Rationale: To assess for baseline orthostatic hypotension, a common side effect of dopaminergic therapy.

Timing: Prior to initiation of therapy.

Complete Blood Count (CBC)

Rationale: To establish baseline hematologic parameters.

Timing: Prior to initiation of therapy.

📊

Routine Monitoring

Motor Symptoms (e.g., dyskinesia, 'on-off' fluctuations)

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.

Blood Pressure (sitting and standing)

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.

Mental Status and Behavioral Changes (e.g., hallucinations, confusion, impulse control disorders)

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.

Liver Function Tests (LFTs)

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.

đŸ‘ī¸

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:

First Trimester: Potential for developmental toxicity observed in animal studies.
Second Trimester: Potential for developmental toxicity observed in animal studies.
Third Trimester: Potential for developmental toxicity observed in animal studies; may inhibit lactation.
🤱

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.

Infant Risk: Moderate risk (L3). Potential for central nervous system effects in the infant due to levodopa. May also inhibit lactation.
đŸ‘ļ

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)
💰

Cost & Coverage

Average Cost: Varies widely, typically $300-$800+ per 30 tablets
Generic Available: Yes
Insurance Coverage: Often Tier 2 or 3, may require prior authorization depending on insurance plan.
📚

General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.