Carbidopa/lev/entac 12.5-50-200mg T
It is used to treat Parkinson's disease.
Drug Class
Anti-Parkinsonian agent
Pharmacologic Class
Dopamine precursor; DOPA decarboxylase inhibitor; Catechol-O-methyltransferase (COMT) inhibitor
Pregnancy Category
Category C
FDA Approved
Jan 2003
DEA Schedule
Not Controlled
Overview
What is this medicine?
This medicine combines three drugs to help manage Parkinson's disease symptoms, especially when your current medication isn't working as well as it used to. Levodopa helps replace a natural chemical in your brain called dopamine. Carbidopa helps more of the levodopa get to your brain and reduces side effects. Entacapone helps the levodopa last longer in your body, which can reduce 'off' times (when your symptoms return).
How to Use This Medicine
Taking Your Medication Correctly
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 in relation to 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 eating acidic foods, may reduce absorption. Discuss your diet with your doctor, especially if you plan to make any changes.
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 advise 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 monitoring your condition. Take this medication at the same time every day, as directed by your doctor or healthcare provider, even if you feel well.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Keep all medications 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. If you have questions about disposing of your medication, consult your pharmacist. You may also want to check if there are any drug take-back programs in your area.
What to Do If You Miss a Dose
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 dosing schedule. Do not take two doses at the same time or take extra doses.
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 in relation to 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 eating acidic foods, may reduce absorption. Discuss your diet with your doctor, especially if you plan to make any changes.
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 advise 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 monitoring your condition. Take this medication at the same time every day, as directed by your doctor or healthcare provider, even if you feel well.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom. Keep all medications 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. If you have questions about disposing of your medication, consult your pharmacist. You may also want to check if there are any drug take-back programs in your area.
What to Do If You Miss a Dose
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 dosing schedule. Do not take two doses at the same time or take extra doses.
Lifestyle & Tips
- Take this medication exactly as prescribed by your doctor. Do not stop taking it suddenly without consulting your doctor, as this can lead to serious withdrawal symptoms.
- Take with a full glass of water. You can take it with or without food, but avoid high-protein meals close to your dose, as protein can reduce the absorption of levodopa.
- Do not crush, chew, or split the tablets. Swallow them whole.
- Be aware that your urine, sweat, or saliva may turn reddish-brown or dark, which is a harmless side effect of entacapone.
- Rise slowly from a sitting or lying position to minimize dizziness or lightheadedness due to orthostatic hypotension.
- Report any new or worsening involuntary movements (dyskinesia), hallucinations, confusion, or unusual urges (e.g., gambling, shopping, eating) to your doctor immediately.
- Avoid driving or operating machinery until you know how this medication affects you, as it can cause drowsiness or sudden sleep onset.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Individualized, typically 1 tablet of Carbidopa/Levodopa/Entacapone 12.5-50-200mg up to 8 times daily, not to exceed 1600mg of entacapone per day.
Dose Range:
1 - 8 mg
Condition-Specific Dosing:
initialTherapy:
Patients already on carbidopa/levodopa and entacapone: switch to the nearest equivalent dose. Patients on carbidopa/levodopa only: initiate with a dose that provides equivalent levodopa, adding entacapone 200mg with each dose. The 12.5-50-200mg strength is often used for patients requiring lower levodopa doses or as part of a titration strategy.
maintenanceTherapy:
Adjust dose and frequency based on clinical response and tolerability, aiming for the lowest effective dose. Max entacapone dose is 1600 mg/day (8 tablets of 200mg entacapone strength).
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but monitor for adverse effects.
Moderate:
No specific dose adjustment recommended, but monitor for adverse effects.
Severe:
Use with caution. Entacapone excretion is primarily biliary, but levodopa/carbidopa metabolites are renally cleared. Monitor for adverse effects.
Dialysis:
Not well studied. Use with caution and monitor closely.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
Use with caution. Entacapone is extensively metabolized by the liver. Consider dose reduction or increased dosing interval.
Severe:
Contraindicated or not recommended due to increased exposure to entacapone. Use with extreme caution and significant dose reduction if absolutely necessary.
Pharmacology
Mechanism of Action
Carbidopa/levodopa/entacapone is a combination product used to treat Parkinson's disease. Levodopa is a metabolic precursor of dopamine that crosses the blood-brain barrier (BBB) and is converted to dopamine in the brain, replenishing dopamine levels. Carbidopa is an aromatic L-amino acid decarboxylase (AADC) inhibitor that does not cross the BBB. It inhibits the peripheral conversion of levodopa to dopamine, allowing more levodopa to reach the brain and reducing peripheral side effects. Entacapone is a selective and reversible catechol-O-methyltransferase (COMT) inhibitor that acts peripherally. It prevents the degradation of levodopa by COMT, thereby increasing the bioavailability and prolonging the half-life of levodopa in the plasma, leading to more sustained levodopa levels in the brain.
Pharmacokinetics
Absorption:
Bioavailability:
Levodopa: ~30% (variable); Carbidopa: ~58% (variable); Entacapone: ~35% (variable)
Tmax:
Levodopa: 0.5-2 hours; Carbidopa: 0.5-2 hours; Entacapone: 0.5-2 hours
FoodEffect:
High-protein meals can significantly reduce the absorption of levodopa, leading to decreased plasma concentrations and potentially reduced efficacy. Entacapone absorption is not significantly affected by food.
Distribution:
Vd:
Levodopa: 0.9-1.6 L/kg; Carbidopa: 1.1 L/kg; Entacapone: 0.27 L/kg (at steady state)
ProteinBinding:
Levodopa: ~10-30%; Carbidopa: ~36%; Entacapone: >98% (primarily to albumin)
CnssPenetration:
Levodopa: Yes (actively transported); Carbidopa: No (does not cross BBB); Entacapone: Limited (does not cross BBB significantly)
Elimination:
HalfLife:
Levodopa: ~1-2 hours (when given with carbidopa); Carbidopa: ~2 hours; Entacapone: ~0.4-0.7 hours (initial), ~2.4 hours (terminal)
Clearance:
Levodopa: ~0.5 L/kg/hr; Carbidopa: Not readily available; Entacapone: ~0.6 L/min
ExcretionRoute:
Levodopa: Primarily renal (metabolites); Carbidopa: Primarily renal (metabolites); Entacapone: Primarily fecal (90-95%), minor renal (10-20%)
Unchanged:
Levodopa: <1% (renal); Carbidopa: ~30% (renal); Entacapone: <0.2% (renal)
Pharmacodynamics
OnsetOfAction:
Variable, typically within 30-60 minutes for levodopa effect.
PeakEffect:
Variable, typically 1-2 hours after dose.
DurationOfAction:
Variable, typically 2-4 hours, but entacapone extends levodopa's half-life, potentially prolonging its effect and reducing 'wearing-off' periods.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
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 behavior 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
Skin lumps or growths
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, uncontrollable sleepiness, including falling asleep 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. Contact your doctor immediately if you experience sudden sleepiness or feel extremely sleepy.
Neuroleptic Malignant Syndrome (NMS)
NMS is a rare but potentially life-threatening condition that can occur when this medication is stopped suddenly or when the dose is lowered. Contact your doctor immediately if you experience any of the following symptoms:
Fever
Muscle cramps or stiffness
Dizziness
Severe headache
Confusion
Changes in thinking
Fast or irregular heartbeat
Excessive sweating
Other Side Effects
Most people do not experience serious 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 go away:
Dizziness
Drowsiness
Fatigue
Weakness
Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Dry mouth
Headache
Trouble sleeping
* Back pain
Reporting Side Effects
If you have questions about side effects or experience any side effects not listed here, contact 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 experience any of the following symptoms, contact your doctor or seek medical attention right away:
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 behavior 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
Skin lumps or growths
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, uncontrollable sleepiness, including falling asleep 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. Contact your doctor immediately if you experience sudden sleepiness or feel extremely sleepy.
Neuroleptic Malignant Syndrome (NMS)
NMS is a rare but potentially life-threatening condition that can occur when this medication is stopped suddenly or when the dose is lowered. Contact your doctor immediately if you experience any of the following symptoms:
Fever
Muscle cramps or stiffness
Dizziness
Severe headache
Confusion
Changes in thinking
Fast or irregular heartbeat
Excessive sweating
Other Side Effects
Most people do not experience serious 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 go away:
Dizziness
Drowsiness
Fatigue
Weakness
Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Dry mouth
Headache
Trouble sleeping
* Back pain
Reporting Side Effects
If you have questions about side effects or experience any side effects not listed here, contact 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 or persistent diarrhea (especially if accompanied by fever or abdominal pain)
- New or worsening involuntary movements (dyskinesia)
- Hallucinations, delusions, confusion, or other psychiatric changes
- Unusual urges or behaviors (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating)
- Sudden onset of sleep during daily activities
- Severe dizziness or fainting spells
- Unexplained muscle pain, tenderness, or weakness (could indicate rhabdomyolysis)
- Yellowing of skin or eyes (jaundice), dark urine, or pale stools (signs of liver problems)
- Signs of neuroleptic malignant syndrome (NMS) if medication is stopped abruptly: fever, rigid muscles, confusion, sweating, fast or irregular heartbeat.
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, health problems, and concerns with your doctor and pharmacist. This includes:
All prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Your doctor needs to assess whether it is safe for you to take this medication in combination with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to ensure your safety.
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, health problems, and concerns with your doctor and pharmacist. This includes:
All prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Your doctor needs to assess whether it is safe for you to take this medication in combination with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to ensure your safety.
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 ensure they have a complete understanding of your treatment plan.
To minimize the risk of accidents, avoid driving and other activities that require alertness until you understand how this medication affects you. When changing positions, such as standing up from a sitting or lying down position, do so slowly to reduce the likelihood of dizziness or fainting. Be cautious when navigating stairs to prevent falls.
Regular blood tests and other laboratory evaluations are crucial to monitor your condition. Adhere to your doctor's schedule for these tests, as this medication may impact the results of certain lab tests. Inform all your healthcare providers and laboratory personnel that you are taking this medication to ensure accurate test results.
You may experience a decrease in the medication's effectiveness as the time approaches for your next dose. If this occurs and causes concern, discuss it with your doctor. It may take several months to realize the full benefits 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. These substances may interact with your medication and increase the risk of adverse effects.
You may notice a dark discoloration (red, brown, or black) in your saliva, urine, or sweat. 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, which can be serious complications.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor. They will discuss the potential benefits and risks of this medication to you and your baby, allowing you to make an informed decision about your treatment.
To minimize the risk of accidents, avoid driving and other activities that require alertness until you understand how this medication affects you. When changing positions, such as standing up from a sitting or lying down position, do so slowly to reduce the likelihood of dizziness or fainting. Be cautious when navigating stairs to prevent falls.
Regular blood tests and other laboratory evaluations are crucial to monitor your condition. Adhere to your doctor's schedule for these tests, as this medication may impact the results of certain lab tests. Inform all your healthcare providers and laboratory personnel that you are taking this medication to ensure accurate test results.
You may experience a decrease in the medication's effectiveness as the time approaches for your next dose. If this occurs and causes concern, discuss it with your doctor. It may take several months to realize the full benefits 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. These substances may interact with your medication and increase the risk of adverse effects.
You may notice a dark discoloration (red, brown, or black) in your saliva, urine, or sweat. 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, which can be serious complications.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor. They will discuss the potential benefits and risks of this medication to you and your baby, allowing you to make an informed decision about your treatment.
Overdose Information
Overdose Symptoms:
- Severe dyskinesia
- Agitation, confusion, hallucinations
- Orthostatic hypotension
- Tachycardia, arrhythmias
- Nausea, vomiting
- Muscle rigidity
What to Do:
Seek immediate medical attention. Call 911 or your local poison control center (1-800-222-1222 in the US). Treatment is supportive, including gastric lavage, IV fluids, and careful monitoring of vital signs and cardiac rhythm. Antiarrhythmics may be needed for cardiac dysrhythmias.
Drug Interactions
Contraindicated Interactions
- Non-selective monoamine oxidase inhibitors (MAOIs) (e.g., phenelzine, tranylcypromine) - risk of hypertensive crisis. Must discontinue MAOIs at least 2 weeks prior to initiating carbidopa/levodopa/entacapone.
Major Interactions
- Selective MAO-B inhibitors (e.g., selegiline, rasagiline) - may increase risk of orthostatic hypotension. Dose reduction of levodopa may be necessary.
- Antipsychotics (e.g., phenothiazines, butyrophenones, risperidone) - may antagonize the effects of levodopa due to dopamine receptor blockade, worsening Parkinson's symptoms.
- Antihypertensives - increased risk of orthostatic hypotension.
- Iron salts (ferrous sulfate, gluconate) - chelation with levodopa and entacapone, reducing absorption of both. Separate administration by at least 2-3 hours.
- Metoclopramide - may antagonize levodopa effect and increase risk of dyskinesia.
- Dopamine D2 receptor antagonists (e.g., domperidone) - may reduce levodopa efficacy.
Moderate Interactions
- Tricyclic antidepressants (TCAs) - may increase risk of orthostatic hypotension and hypertension.
- Sympathomimetics (e.g., epinephrine, norepinephrine, isoproterenol) - increased risk of arrhythmias and hypertension.
- Other drugs metabolized by COMT (e.g., isoproterenol, epinephrine, norepinephrine, dopamine, dobutamine, alpha-methyldopa, apomorphine) - entacapone may inhibit their metabolism, increasing their effects.
- Protein-rich foods - can reduce levodopa absorption.
Minor Interactions
- Antacids - may slightly increase levodopa absorption.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC)
Rationale: To establish baseline and monitor for potential hematologic abnormalities (e.g., hemolytic anemia, thrombocytopenia, leukopenia) associated with levodopa/carbidopa.
Timing: Prior to initiation
Liver Function Tests (LFTs)
Rationale: To establish baseline and monitor for potential hepatotoxicity, especially with entacapone.
Timing: Prior to initiation
Renal Function Tests (RFTs)
Rationale: To establish baseline and guide dosing in patients with renal impairment.
Timing: Prior to initiation
Blood Pressure (BP) and Heart Rate (HR)
Rationale: To establish baseline and monitor for orthostatic hypotension.
Timing: Prior to initiation (supine and standing)
Mental Status/Cognitive Assessment
Rationale: To establish baseline for monitoring psychiatric side effects (e.g., hallucinations, confusion, impulse control disorders).
Timing: Prior to initiation
Routine Monitoring
Clinical response to Parkinson's symptoms (motor fluctuations, dyskinesia)
Frequency: Regularly, at each visit or as needed for dose adjustment
Target: Improved motor function, reduced 'off' time, manageable dyskinesia
Action Threshold: Worsening symptoms, increased 'off' time, troublesome dyskinesia, or new psychiatric symptoms warrant dose adjustment or re-evaluation.
Blood Pressure (BP) and Heart Rate (HR)
Frequency: Regularly, especially during dose titration and if symptoms of orthostatic hypotension occur.
Target: Within patient's normal range, without significant orthostatic drop.
Action Threshold: Significant orthostatic drop (>20 mmHg systolic or >10 mmHg diastolic) or symptomatic hypotension.
Mental Status/Psychiatric symptoms (hallucinations, delusions, confusion, impulse control disorders)
Frequency: Regularly, at each visit.
Target: Absence or manageable level of psychiatric symptoms.
Action Threshold: New onset or worsening of psychiatric symptoms, requiring dose adjustment or addition of adjunctive therapy.
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 of liver enzymes (e.g., >3x ULN).
CBC
Frequency: Periodically, especially if patient develops unexplained fever, sore throat, or other signs of infection.
Target: Within normal limits.
Action Threshold: Significant abnormalities (e.g., leukopenia, thrombocytopenia, hemolytic anemia).
Symptom Monitoring
- Orthostatic hypotension (dizziness, lightheadedness upon standing)
- Dyskinesia (involuntary movements)
- Nausea, vomiting, diarrhea, abdominal pain
- Hallucinations, delusions, confusion, psychosis
- Impulse control disorders (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating)
- Sleep disturbances (insomnia, somnolence, sudden onset of sleep)
- Urine discoloration (orange-brown)
- Diarrhea (can be severe and persistent with entacapone)
- Rhabdomyolysis (rare, but monitor for muscle pain, weakness, dark urine)
Special Patient Groups
Pregnancy
Use during pregnancy should be avoided unless the potential benefit justifies the potential risk to the fetus. Levodopa has shown developmental toxicity in animal studies. Entacapone has shown some evidence of embryotoxicity in animal studies at high doses.
Trimester-Specific Risks:
First Trimester:
Potential for developmental toxicity based on animal studies. Avoid if possible.
Second Trimester:
Potential for developmental toxicity. Use only if clearly needed.
Third Trimester:
Potential for developmental toxicity. Use only if clearly needed. May affect fetal heart rate and movement.
Lactation
Levodopa is excreted in human milk and may inhibit lactation. Entacapone is excreted in animal 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:
L3 - Moderate risk. Potential for inhibition of lactation, and unknown effects of levodopa and entacapone on the infant. Monitor infant for drowsiness, poor feeding, and motor changes.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients. Not recommended for use in this population.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Elderly patients may be more susceptible to certain adverse effects such as hallucinations, confusion, and orthostatic hypotension. Dose titration should be done carefully.
Clinical Information
Clinical Pearls
- This combination is particularly useful for patients experiencing 'wearing-off' phenomena with carbidopa/levodopa alone, as entacapone helps to extend the duration of levodopa's effect.
- Patients should be advised about the harmless discoloration of urine, sweat, and saliva (orange-brown) due to entacapone.
- Monitor for impulse control disorders (ICDs) such as pathological gambling, hypersexuality, and compulsive shopping, which can occur with dopaminergic therapies. Patients and caregivers should be educated to recognize these.
- Sudden onset of sleep can occur without warning; advise patients to avoid driving or activities requiring alertness if this occurs.
- Diarrhea is a common side effect of entacapone and can be severe and persistent. If severe diarrhea occurs, consider discontinuation of entacapone.
- Avoid abrupt discontinuation of this medication, as it can lead to a symptom complex resembling neuroleptic malignant syndrome (NMS), characterized by fever, muscle rigidity, altered mental status, and autonomic instability.
Alternative Therapies
- Dopamine agonists (e.g., pramipexole, ropinirole, rotigotine, apomorphine)
- MAO-B inhibitors (e.g., selegiline, rasagiline, safinamide)
- COMT inhibitors (e.g., tolcapone, opicapone - if entacapone is not tolerated or ineffective)
- Amantadine (for dyskinesia or motor fluctuations)
- Istradefylline (adenosine A2A receptor antagonist)
- Pimavanserin (for Parkinson's disease psychosis)
Cost & Coverage
Average Cost:
$100 - $500+ per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (for generic), Tier 3 or Tier 4 (for brand)
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 this 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.