Requip XL 2mg Tablets

Manufacturer GLAXO SMITH KLINE Active Ingredient Ropinirole Extended-Release Tablets(roe PIN i role) Pronunciation ROE-pin-i-role
It is used to treat Parkinson's disease.
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Drug Class
Anti-Parkinsonian Agent
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Pharmacologic Class
Dopamine Agonist
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Pregnancy Category
Category C
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FDA Approved
Jun 2007
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Ropinirole extended-release is a medication used to treat Parkinson's disease. It works by acting like a natural chemical in your brain called dopamine, which helps control movement. The extended-release form means it's designed to release the medicine slowly over 24 hours, so you only need to take it once a day.
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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 the medication with or without food, and swallow the tablet whole - do not chew, break, or crush it. If you have a condition like diarrhea that causes the medication to pass through your body too quickly, you may notice what appears to be the tablet in your stool. If this happens, consult your doctor.

Continue taking the medication as directed by your doctor or healthcare provider, even if you're feeling well. If you need to stop taking the medication, discuss this with your doctor first. You may need to restart at a lower dose and gradually increase it.

Storing and Disposing of Your Medication

Store the medication at room temperature, protected from light and moisture. Keep the container tightly closed and store it in a dry place, away from the bathroom. Keep all medications 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. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs.

Missing a Dose

If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses. If you miss several days of medication, consult your doctor for instructions on how to restart your treatment.
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Lifestyle & Tips

  • Take the tablet whole; do not crush, chew, or divide it.
  • Take at approximately the same time each day, with or without food.
  • Be aware of potential for sudden sleep onset; avoid driving or operating machinery if you experience drowsiness or sleep attacks.
  • Rise slowly from a sitting or lying position to minimize dizziness from low blood pressure.
  • Report any new or unusual urges or behaviors (e.g., gambling, increased sexual urges, compulsive shopping, binge eating) to your doctor.
  • Avoid alcohol or other sedating medications, as they can worsen drowsiness.

Dosing & Administration

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Adult Dosing

Standard Dose: Initial 2 mg once daily for Parkinson's Disease, titrated weekly.
Dose Range: 2 - 24 mg

Condition-Specific Dosing:

Parkinson's Disease: Initial: 2 mg orally once daily for 1 week. Titration: Increase by 2 mg/day at weekly intervals up to 12 mg/day. If needed, may further increase by 2 mg/day to 4 mg/day at weekly or longer intervals up to a maximum of 24 mg/day. Doses should be taken at approximately the same time each day, with or without food.
Switching from immediate-release ropinirole: Patients may be switched overnight from immediate-release ropinirole to Requip XL. The total daily dose of Requip XL should be equivalent to the total daily dose of immediate-release ropinirole.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
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Dose Adjustments

Renal Impairment:

Mild: No dosage adjustment required (CrCl 30-50 mL/min)
Moderate: No dosage adjustment required (CrCl 30-50 mL/min)
Severe: Consider dosage reduction in patients with end-stage renal disease (CrCl <30 mL/min) on hemodialysis. Maximum recommended dose is 18 mg/day.
Dialysis: Supplemental doses are not needed after routine hemodialysis.

Hepatic Impairment:

Mild: Not available
Moderate: Use with caution. No specific dosage recommendations are available, but ropinirole is extensively metabolized by the liver.
Severe: Use with caution. No specific dosage recommendations are available, but ropinirole is extensively metabolized by the liver.

Pharmacology

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Mechanism of Action

Ropinirole is a non-ergoline dopamine agonist with high affinity for D2 and D3 dopamine receptors. It is believed to stimulate postsynaptic D2-type receptors in the caudate-putamen in the brain, thereby mimicking the effects of dopamine and alleviating the motor symptoms of Parkinson's disease.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 55%
Tmax: 6-10 hours (extended-release)
FoodEffect: Food does not affect the AUC or Cmax of ropinirole extended-release tablets, but Tmax may be prolonged by approximately 2.5 hours.

Distribution:

Vd: Approximately 7.5 L/kg
ProteinBinding: Approximately 35-40%
CnssPenetration: Yes

Elimination:

HalfLife: Approximately 6 hours (extended-release)
Clearance: Approximately 47 L/hr (oral clearance)
ExcretionRoute: Primarily renal (approximately 60% as metabolites)
Unchanged: Less than 10% (as unchanged drug in urine)
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Pharmacodynamics

OnsetOfAction: Gradual (due to extended-release formulation and titration)
PeakEffect: Not precisely defined for therapeutic effect, but plasma concentration peaks at 6-10 hours.
DurationOfAction: 24 hours (extended-release)

Safety & Warnings

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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 or seek immediate 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
Signs of high or low blood pressure, including:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Signs of a urinary tract infection (UTI), such as:
+ Blood in the urine
+ Burning or pain while urinating
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain or pelvic pain
Confusion, difficulty focusing, or changes in behavior
Strong, uncontrollable urges (e.g., eating, gambling, sex, or spending money)
Changes in eyesight
Chest pain or pressure
Abnormal heartbeat (fast, slow, or irregular)
Hallucinations (seeing or hearing things that are not there)
Mood changes
Shortness of breath
New or worsening trouble controlling body movements
Swelling
Burning, numbness, or tingling sensations that are not normal
Memory problems or loss
Fever
Muscle stiffness
Sudden, unexplained sleepiness, especially during activities like driving, eating, or talking. If this occurs, do not drive or engage in tasks that require alertness while taking this medication. Contact your doctor immediately if you experience excessive sleepiness.

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:

Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Dizziness
Sleepiness
Fatigue
Weakness
Headache
Excessive sweating
Dry mouth
Joint pain
Nervousness or excitability
Shakiness
Anxiety
Nose or throat irritation
Back pain

This list is not exhaustive. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Sudden onset of sleep during daily activities
  • Severe dizziness or fainting, especially when standing up
  • Hallucinations (seeing or hearing things that are not real)
  • Uncontrolled, involuntary movements (dyskinesia)
  • New or increased urges to gamble, shop, eat, or engage in sexual activity
  • Unexplained swelling in the legs or ankles
  • Severe nausea or vomiting
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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 symptoms you experienced.
If you are currently taking another medication that contains the same active ingredient as this drug.
Potential interactions with other medications or health conditions. To ensure safe use, disclose all your medications, including:
+ Prescription and over-the-counter (OTC) drugs
+ Natural products
+ Vitamins
Any existing health problems, as they may affect the safety of taking this medication.

Remember to consult with your doctor before making any changes to your medication regimen, including starting, stopping, or adjusting the dose of any drug. This will help ensure your safety and the effectiveness of your treatment.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

To ensure your safety, 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 minimize the risk of dizziness or fainting. Be cautious when navigating stairs.

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 guidance provided by your doctor. Be aware of potential withdrawal symptoms, which may include fever, confusion, severe muscle stiffness, apathy, anxiety, depression, fatigue, sleep disturbances, sweating, or pain. If you experience any of these symptoms when reducing the dose or stopping the medication, contact your doctor immediately.

If you start or stop smoking, notify your doctor, as this may necessitate an adjustment in your medication dosage. Before consuming alcohol, marijuana, or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions, consult with your doctor.

Monitor your blood pressure and heart rate as directed by your doctor. Be aware of the risk of neuroleptic malignant syndrome (NMS), a potentially life-threatening condition that may occur when medications like this one are stopped suddenly or when the dose is lowered. If you experience symptoms such as fever, muscle cramps or stiffness, dizziness, severe headache, confusion, altered mental status, rapid or abnormal heartbeat, or excessive sweating, contact your doctor right away.

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant or breastfeeding women, or those planning to become pregnant, should discuss the benefits and risks of this medication with their doctor to make an informed decision.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Dizziness
  • Somnolence
  • Orthostatic hypotension
  • Sweating
  • Palpitations
  • Chest pain
  • Confusion
  • Psychosis

What to Do:

Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Management is supportive, including maintaining blood pressure and treating symptoms.

Drug Interactions

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Major Interactions

  • CYP1A2 inhibitors (e.g., ciprofloxacin, fluvoxamine): May increase ropinirole exposure, requiring dose reduction.
  • Dopamine antagonists (e.g., antipsychotics like haloperidol, phenothiazines, metoclopramide): May reduce the efficacy of ropinirole.
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Moderate Interactions

  • Estrogens (e.g., hormone replacement therapy): May decrease ropinirole clearance, potentially increasing exposure. Dose adjustment may be needed.
  • Smoking: Induces CYP1A2, potentially increasing ropinirole clearance and decreasing exposure. Dose adjustment may be needed in smokers who start or stop smoking.

Monitoring

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Baseline Monitoring

Blood Pressure (sitting and standing)

Rationale: To assess for baseline orthostatic hypotension risk.

Timing: Before initiation of therapy

Renal function (CrCl)

Rationale: To guide dosing in severe renal impairment.

Timing: Before initiation of therapy

Mental status/Psychiatric history

Rationale: To assess for risk of impulse control disorders, hallucinations, or psychosis.

Timing: Before initiation of therapy

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Routine Monitoring

Blood Pressure (sitting and standing)

Frequency: Regularly, especially during dose titration and if symptoms of orthostatic hypotension occur.

Target: Maintain within patient's normal range, minimize symptomatic drops.

Action Threshold: Symptomatic orthostatic hypotension (e.g., dizziness, syncope) or significant drop (e.g., >20 mmHg systolic, >10 mmHg diastolic) upon standing.

Motor symptoms of Parkinson's Disease

Frequency: Regularly during follow-up visits.

Target: Improvement in bradykinesia, rigidity, tremor.

Action Threshold: Worsening symptoms, inadequate response to current dose.

Sleep patterns/Daytime somnolence

Frequency: Regularly, inquire about sudden sleep onset.

Target: Normal sleep patterns, no excessive daytime sleepiness.

Action Threshold: Reports of sudden sleep onset, excessive daytime somnolence, or sleep attacks.

Behavioral changes/Impulse control disorders

Frequency: Regularly, inquire about new or worsening compulsive behaviors (e.g., gambling, hypersexuality, binge eating, compulsive shopping).

Target: Absence of new or worsening compulsive behaviors.

Action Threshold: Patient or caregiver reports of new or worsening compulsive behaviors.

Dyskinesia

Frequency: Regularly, especially if co-administered with levodopa.

Target: Minimize or prevent dyskinesia.

Action Threshold: Development or worsening of dyskinesia.

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Symptom Monitoring

  • Orthostatic hypotension (dizziness, lightheadedness, fainting upon standing)
  • Excessive daytime sleepiness or sudden sleep onset
  • Hallucinations (visual, auditory)
  • Dyskinesia (involuntary movements)
  • Impulse control disorders (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating)
  • Nausea, vomiting, abdominal pain
  • Peripheral edema

Special Patient Groups

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Pregnancy

Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects, but there are no adequate and well-controlled studies in pregnant women.

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.
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Lactation

Ropinirole is expected to inhibit lactation due to its dopamine agonist activity. It is unknown if ropinirole is excreted in human milk. 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 inhibition of lactation; unknown direct infant exposure or effects.
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Pediatric Use

Safety and effectiveness in pediatric patients have not been established. Not recommended for use in this population.

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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. Start with the lowest effective dose and titrate slowly, monitoring for adverse effects, particularly orthostatic hypotension and hallucinations.

Clinical Information

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Clinical Pearls

  • Ropinirole ER is taken once daily, offering convenience compared to the immediate-release formulation.
  • Patients should be warned about the potential for sudden onset of sleep, even without prior warning signs of drowsiness. This can occur at any time during daily activities.
  • Impulse control disorders (e.g., pathological gambling, hypersexuality, compulsive shopping, binge eating) are a known side effect of dopamine agonists. Patients and caregivers should be educated to recognize and report these behaviors.
  • Orthostatic hypotension is common, especially during initiation and dose titration. Advise patients to rise slowly.
  • Hallucinations are more common in elderly patients and those with advanced Parkinson's disease, especially when used with levodopa.
  • Do not crush, chew, or divide Requip XL tablets, as this will alter the extended-release properties and may lead to rapid drug release and increased side effects.
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Alternative Therapies

  • Pramipexole (Mirapex, Mirapex ER)
  • Rotigotine (Neupro patch)
  • Levodopa/Carbidopa (Sinemet, Rytary, Duopa)
  • Other dopamine agonists (e.g., bromocriptine, apomorphine)
  • MAO-B inhibitors (e.g., selegiline, rasagiline, safinamide)
  • COMT inhibitors (e.g., entacapone, opicapone)
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Cost & Coverage

Average Cost: Varies widely, typically $100-$500+ per 30 tablets
Generic Available: Yes
Insurance Coverage: Often Tier 2 or 3, depending on insurance plan and formulary.
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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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.