Pramipexole ER 4.5mg Tablets
It is used to treat Parkinson's disease.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Anti-Parkinson's agent
Pharmacologic Class
Dopamine agonist, non-ergot
Pregnancy Category
Category C
FDA Approved
May 2009
DEA Schedule
Not Controlled
Overview
What is this medicine?
Pramipexole ER is an extended-release tablet used to treat Parkinson's disease and restless legs syndrome. It works by acting like a natural chemical in your brain called dopamine, which helps control movement.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. If it causes stomach upset, take it with food to help minimize this side effect. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
It's essential to swallow the medication whole and not chew, break, or crush it. This will help ensure you receive the correct dose and minimize the risk of side effects.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature, protected from light and moisture. Avoid storing it in a bathroom or any area prone to high humidity. Keep all medications in a secure location, out of the reach of children and pets.
When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist or healthcare provider. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore local 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 has been 12 hours or more since the missed dose, skip it 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. If you miss taking your medication for several days in a row, contact your doctor before restarting your medication regimen.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. If it causes stomach upset, take it with food to help minimize this side effect. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
It's essential to swallow the medication whole and not chew, break, or crush it. This will help ensure you receive the correct dose and minimize the risk of side effects.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature, protected from light and moisture. Avoid storing it in a bathroom or any area prone to high humidity. Keep all medications in a secure location, out of the reach of children and pets.
When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist or healthcare provider. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore local 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 has been 12 hours or more since the missed dose, skip it 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. If you miss taking your medication for several days in a row, contact your doctor before restarting your medication regimen.
Lifestyle & Tips
- Take the tablet whole; do not crush, chew, or divide it.
- Take with or without food, at the same time each day.
- Avoid sudden changes in position (e.g., standing up quickly) to reduce dizziness or lightheadedness.
- Be cautious when driving or operating machinery, as this medication can cause sudden sleep onset without warning.
- Avoid alcohol and other sedating medications, as they can increase drowsiness.
- Report any new or unusual urges or behaviors (e.g., gambling, increased sexual urges, compulsive shopping, binge eating) to your doctor immediately.
Available Forms & Alternatives
Available Strengths:
- Pramipexole 0.5mg Tablets
- Pramipexole 0.25mg Tablets
- Pramipexole 1mg Tablets
- Pramipexole 1.5mg Tablets
- Pramipexole 0.125mg Tablets
- Pramipexole 0.75mg Tablets
- Pramipexole ER 4.5mg Tablets
- Pramipexole ER 1.5mg Tablets
- Pramipexole ER 3mg Tablets
- Pramipexole ER 0.375mg Tablets
- Pramipexole ER 0.75mg Tablets
- Pramipexole ER 0.75mg Tablets
- Pramipexole ER 0.375mg Tablets
- Pramipexole ER 1.5mg Tablets
- Pramipexole ER 3.75mg Tablets
- Pramipexole ER 4.5mg Tablets
- Pramipexole ER 3mg Tablets
- Pramipexole ER 2.25mg Tablets
Dosing & Administration
Adult Dosing
Standard Dose:
For Parkinson's Disease: Initial 0.375 mg once daily, titrated gradually to a target dose of 1.5 mg to 4.5 mg once daily. The 4.5 mg dose is the maximum recommended daily dose.
Dose Range:
0.375 - 4.5 mg
Condition-Specific Dosing:
Parkinson's Disease:
Initial 0.375 mg once daily, increase by 0.375 mg no more frequently than every 5-7 days to a maximum of 4.5 mg once daily.
Restless Legs Syndrome (RLS):
Initial 0.125 mg once daily, increase by 0.125 mg no more frequently than every 4-7 days to a maximum of 2.25 mg once daily. (Note: 4.5mg is not a typical RLS dose)
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
CrCl 30-50 mL/min: Initial 0.375 mg every other day. Max dose 2.25 mg once daily.
Moderate:
CrCl 15-29 mL/min: Initial 0.375 mg twice a week. Max dose 1.5 mg once daily.
Severe:
CrCl <15 mL/min: Not recommended.
Dialysis:
Not recommended for patients on dialysis.
Hepatic Impairment:
Mild:
No adjustment needed.
Moderate:
No adjustment needed.
Severe:
No adjustment needed.
Pharmacology
Mechanism of Action
Pramipexole is a non-ergot dopamine agonist with high affinity and selectivity for the D2 subfamily of dopamine receptors, with preferential binding to D3 receptor subtypes. It is thought to exert its therapeutic effects by stimulating dopamine receptors in the striatum.
Pharmacokinetics
Absorption:
Bioavailability:
>90%
Tmax:
6 hours (range 3-10 hours) for ER formulation
FoodEffect:
Food does not affect the extent of absorption, but Tmax may be prolonged by approximately 2 hours.
Distribution:
Vd:
Approximately 400 L
ProteinBinding:
<20%
CnssPenetration:
Yes
Elimination:
HalfLife:
8-12 hours (increases with age and renal impairment)
Clearance:
Approximately 400 mL/min (renal clearance)
ExcretionRoute:
Renal
Unchanged:
>90%
Pharmacodynamics
OnsetOfAction:
Gradual, typically weeks for full therapeutic effect in Parkinson's disease due to titration.
PeakEffect:
Correlates with Tmax (6 hours for ER).
DurationOfAction:
24 hours (due to extended-release formulation).
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
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Strong, uncontrollable urges (e.g., eating, gambling, sex, or spending money)
Fever
Confusion
Muscle stiffness
Increased urination
Severe dizziness or fainting
Excessive sweating
Shortness of breath, significant weight gain, or swelling in the arms or legs
Changes in vision
New or worsening trouble controlling body movements
Difficulty moving around
Hallucinations (seeing or hearing things that are not there)
Memory problems or loss
Muscle pain or weakness, dark urine, or difficulty urinating
New or worsening mental, mood, or behavioral changes
Some people have experienced sudden, uncontrollable sleepiness, even during activities like driving, eating, or talking, up to 1 year after starting this medication. If this happens to you, do not drive or engage in activities that require alertness. Contact your doctor immediately if you experience excessive sleepiness or fall asleep during activities.
Additionally, some people have developed uncontrolled changes in posture, such as neck bending forward, bending forward at the waist, or tilting sideways while sitting, standing, or walking. These changes may occur several months after starting the medication or after a dose increase. If you notice any changes in your posture, contact your doctor.
Neuroleptic Malignant Syndrome (NMS): This is a rare but potentially life-threatening condition that can occur when medications like this one are stopped abruptly or when the dose is lowered. If you experience any of the following symptoms, contact your doctor immediately:
Fever
Muscle cramps or stiffness
Dizziness
Severe headache
Confusion
Changes in thinking
Fast or abnormal heartbeat
Excessive sweating
Other Possible Side Effects
While many people do not experience side effects or only have mild ones, it is essential to be aware of the following potential side effects:
Headache
Constipation
Diarrhea
Upset stomach
Decreased appetite
Trouble sleeping
Dizziness
Sleepiness
Fatigue
Weakness
Dry mouth
Strange or vivid dreams
Muscle spasms
Weight loss
Stuffy nose
Flu-like symptoms
If any of these side effects or other symptoms bother you or do not go away, contact your doctor for advice. 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
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Strong, uncontrollable urges (e.g., eating, gambling, sex, or spending money)
Fever
Confusion
Muscle stiffness
Increased urination
Severe dizziness or fainting
Excessive sweating
Shortness of breath, significant weight gain, or swelling in the arms or legs
Changes in vision
New or worsening trouble controlling body movements
Difficulty moving around
Hallucinations (seeing or hearing things that are not there)
Memory problems or loss
Muscle pain or weakness, dark urine, or difficulty urinating
New or worsening mental, mood, or behavioral changes
Some people have experienced sudden, uncontrollable sleepiness, even during activities like driving, eating, or talking, up to 1 year after starting this medication. If this happens to you, do not drive or engage in activities that require alertness. Contact your doctor immediately if you experience excessive sleepiness or fall asleep during activities.
Additionally, some people have developed uncontrolled changes in posture, such as neck bending forward, bending forward at the waist, or tilting sideways while sitting, standing, or walking. These changes may occur several months after starting the medication or after a dose increase. If you notice any changes in your posture, contact your doctor.
Neuroleptic Malignant Syndrome (NMS): This is a rare but potentially life-threatening condition that can occur when medications like this one are stopped abruptly or when the dose is lowered. If you experience any of the following symptoms, contact your doctor immediately:
Fever
Muscle cramps or stiffness
Dizziness
Severe headache
Confusion
Changes in thinking
Fast or abnormal heartbeat
Excessive sweating
Other Possible Side Effects
While many people do not experience side effects or only have mild ones, it is essential to be aware of the following potential side effects:
Headache
Constipation
Diarrhea
Upset stomach
Decreased appetite
Trouble sleeping
Dizziness
Sleepiness
Fatigue
Weakness
Dry mouth
Strange or vivid dreams
Muscle spasms
Weight loss
Stuffy nose
Flu-like symptoms
If any of these side effects or other symptoms bother you or do not go away, contact your doctor for advice. 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:
- Dizziness, lightheadedness, or fainting, especially when standing up (orthostatic hypotension)
- Excessive daytime sleepiness or falling asleep suddenly without warning
- Hallucinations (seeing or hearing things that are not there)
- Unusual urges or behaviors (e.g., compulsive gambling, increased sexual urges, uncontrolled shopping, binge eating)
- Nausea, constipation, or swelling in the legs/ankles
- Involuntary movements (dyskinesia), especially if also taking levodopa
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.
If you have kidney disease, as this may affect how your body processes the medication.
If you are currently taking another medication that contains the same active ingredient as this drug, to avoid potential interactions or duplicate dosing.
This list is not exhaustive, and it is crucial to discuss all your medications, health conditions, and supplements with your doctor and pharmacist. This includes:
All prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Your doctor needs this information to ensure it is safe for you to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor to avoid potential interactions or adverse effects.
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.
If you have kidney disease, as this may affect how your body processes the medication.
If you are currently taking another medication that contains the same active ingredient as this drug, to avoid potential interactions or duplicate dosing.
This list is not exhaustive, and it is crucial to discuss all your medications, health conditions, and supplements with your doctor and pharmacist. This includes:
All prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Your doctor needs this information to ensure it is safe for you to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor to avoid potential interactions or adverse effects.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
When starting this medication, be cautious when driving or performing tasks that require alertness, as it may affect your ability to do so. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying position, and exercise caution when climbing stairs.
Follow your doctor's instructions for monitoring your blood pressure. Do not discontinue this medication without consulting your doctor, as stopping it abruptly may lead to withdrawal symptoms. If you need to stop taking this medication, follow the tapering schedule recommended by your doctor. Immediately contact your doctor if you experience any of the following symptoms when reducing the dose or stopping the medication: fever, confusion, severe muscle stiffness, apathy, anxiety, depression, fatigue, sleep disturbances, sweating, or pain.
Avoid consuming alcohol while taking this medication. Before using marijuana, cannabis products, or prescription or over-the-counter medications that may cause drowsiness, consult with your doctor.
If you notice what appears to be a tablet in your stool, discuss this with your doctor.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
When starting this medication, be cautious when driving or performing tasks that require alertness, as it may affect your ability to do so. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying position, and exercise caution when climbing stairs.
Follow your doctor's instructions for monitoring your blood pressure. Do not discontinue this medication without consulting your doctor, as stopping it abruptly may lead to withdrawal symptoms. If you need to stop taking this medication, follow the tapering schedule recommended by your doctor. Immediately contact your doctor if you experience any of the following symptoms when reducing the dose or stopping the medication: fever, confusion, severe muscle stiffness, apathy, anxiety, depression, fatigue, sleep disturbances, sweating, or pain.
Avoid consuming alcohol while taking this medication. Before using marijuana, cannabis products, or prescription or over-the-counter medications that may cause drowsiness, consult with your doctor.
If you notice what appears to be a tablet in your stool, discuss this with your doctor.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Hyperkinesia (excessive involuntary movements)
- Hallucinations
- Agitation
- Hypotension (low blood pressure)
- Sedation
What to Do:
There is no known antidote. Treatment should be symptomatic and supportive. Gastric lavage may be indicated if ingestion is recent. Maintain blood pressure with intravenous fluids and/or dopamine agonists. Call 1-800-222-1222 (Poison Control Center) immediately.
Drug Interactions
Major Interactions
- Dopamine antagonists (e.g., phenothiazines, butyrophenones, thioxanthenes, metoclopramide): May reduce the efficacy of pramipexole.
Moderate Interactions
- Cimetidine, Ranitidine, Diltiazem, Verapamil, Quinidine, Quinine: May decrease the renal clearance of pramipexole, leading to increased plasma levels.
- Sedatives, Alcohol, other CNS depressants: May potentiate the sedative effects of pramipexole.
Monitoring
Baseline Monitoring
Renal function (CrCl)
Rationale: Pramipexole is primarily renally eliminated; dose adjustment is required in renal impairment.
Timing: Prior to initiation of therapy.
Blood pressure (orthostatic)
Rationale: Risk of orthostatic hypotension, especially at treatment initiation and dose escalation.
Timing: Prior to initiation and periodically during titration.
Psychiatric history (e.g., impulse control disorders, psychosis)
Rationale: Pramipexole can exacerbate or induce impulse control disorders, hallucinations, and psychosis.
Timing: Prior to initiation.
Routine Monitoring
Efficacy (Parkinson's symptoms, RLS symptoms)
Frequency: Periodically, especially during dose titration and maintenance.
Target: Improved motor function, reduced RLS symptoms.
Action Threshold: Lack of improvement or worsening symptoms may indicate need for dose adjustment or alternative therapy.
Blood pressure (orthostatic)
Frequency: Periodically, especially during dose titration.
Target: Stable blood pressure without symptomatic orthostasis.
Action Threshold: Symptomatic orthostatic hypotension (dizziness, lightheadedness, falls) may require dose reduction or discontinuation.
Somnolence/Sudden Sleep Onset
Frequency: Regularly, especially during dose titration.
Target: Absence of excessive daytime sleepiness or sudden sleep attacks.
Action Threshold: Reported somnolence or sudden sleep attacks warrant dose reduction or discontinuation, and patient counseling regarding driving/operating machinery.
Impulse Control Disorders (ICDs)
Frequency: Regularly, inquire about new or increased urges (e.g., gambling, hypersexuality, compulsive shopping, binge eating).
Target: Absence of new or worsening ICDs.
Action Threshold: Development of ICDs requires dose reduction, discontinuation, or consideration of alternative therapy.
Hallucinations/Psychosis
Frequency: Regularly, inquire about visual or auditory hallucinations, delusions.
Target: Absence of new or worsening psychotic symptoms.
Action Threshold: Development of psychotic symptoms requires dose reduction or discontinuation.
Dyskinesia (in Parkinson's)
Frequency: Periodically, especially with concomitant levodopa.
Target: Minimization of involuntary movements.
Action Threshold: Significant dyskinesia may require dose adjustment of pramipexole or levodopa.
Symptom Monitoring
- Orthostatic hypotension (dizziness, lightheadedness, fainting)
- Excessive daytime sleepiness or sudden sleep onset
- Hallucinations (visual, auditory)
- Delusions or paranoid ideation
- New or increased urges (e.g., gambling, hypersexuality, compulsive shopping, binge eating)
- Nausea, constipation
- Peripheral edema
- Dyskinesia (involuntary movements)
Special Patient Groups
Pregnancy
Pramipexole is classified as Pregnancy Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Animal studies show adverse effects on embryo-fetal development at doses higher than human therapeutic doses. Human data are limited.
Second Trimester:
Limited human data; animal studies suggest potential for adverse effects.
Third Trimester:
Limited human data; animal studies suggest potential for adverse effects.
Lactation
Pramipexole is excreted into breast milk and has the potential to inhibit lactation due to its dopamine agonist activity. 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:
Potential for adverse effects in the breastfed infant (e.g., somnolence, feeding difficulties) and inhibition of lactation.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use is not recommended.
Geriatric Use
Renal clearance of pramipexole decreases with age, necessitating dose adjustment in elderly patients with impaired renal function. Elderly patients may also be at increased risk for hallucinations and orthostatic hypotension.
Clinical Information
Clinical Pearls
- Pramipexole ER should be swallowed whole and not crushed, chewed, or divided, as this can lead to rapid release of the drug and increased side effects.
- Titrate dose slowly to minimize side effects such as orthostatic hypotension and somnolence.
- Counsel patients on the risk of sudden sleep attacks and impulse control disorders, and advise them to report these symptoms immediately.
- Monitor for peripheral edema, a common side effect.
- In patients with advanced Parkinson's disease, pramipexole can exacerbate dyskinesia when used concomitantly with levodopa; dose adjustments of either medication may be necessary.
Alternative Therapies
- Other dopamine agonists (e.g., ropinirole, rotigotine, bromocriptine)
- Levodopa/Carbidopa (for Parkinson's Disease)
- MAO-B inhibitors (e.g., selegiline, rasagiline, safinamide)
- COMT inhibitors (e.g., entacapone, opicapone)
- Amantadine
- Adenosine A2A receptor antagonists (e.g., istradefylline)
- Non-pharmacological treatments for RLS (e.g., lifestyle modifications, iron supplementation if deficient)
Cost & Coverage
Average Cost:
Highly variable, typically $50 - $300+ per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic), Tier 3 or higher (for brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is 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 it's a good idea 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 overdose, including the medication taken, the amount, and the time it occurred.