Ropinirole

Ropiniroleis a prescription medication used to treat Parkinson's disease and moderate to severeRestless Leg Syndrome.

• Ropinirole is available under the following different brand names:Requip,Requip XL

Adult dosage

Tablet

• 0.25mg
• 0.5mg
• 1mg
• 2mg
• 3mg
• 4mg
• 5mg

Tablet, extended-release

• 2mg
• 4mg
• 6mg
• 8mg
• 12mg

Parkinson Disease

Adult dosage

Immediate Release

• 0.25 mg orally every 8 hours for 1 week initially, then increased weekly by 0.25 mg every 8 hours; if necessary, after week 4, maybe increased weekly by 1.5mg/day up to 9 mg/day, then increased weekly by 3 mg/day up to 24 mg/day

Extended-release

• 2 mg/day orally initially for 1-2 weeks; increased by 2 mg/day at intervals over 1 week; not to exceed 24 mg/day
• Maximum dose
  • Although the maximum recommended is 24 mg/day, patients with advanced Parkinson disease should generally be maintained at lower doses
  • In fixed-dose studies designed to characterize dose-response, no additional therapeutic benefit was shown in advanced-stage Parkinson disease with doses over 8 mg/day or with early-stage Parkinson disease with doses over 12 mg/day
  • Early Parkinson disease: No more than 12 mg/day
  • Advanced Parkinson disease: No more than 8 mg/day

Restless Leg Syndrome (Moderate-Severe)

Adult dosage

• Immediate-release: 0.25 mg/day orally 1-3 hours before bedtime; after day 2, may be increased to 0.5 mg/day orally; at end of week 1, increased to 1 mg/day, then increased weekly by 0.5 mg/day up to 4 mg/day

Dosage Considerations – Should be Given as Follows:

• See “Dosages”.

Common side effects of Ropinirole include:

• drowsiness,
• dizziness,
• weakness,
• headache,
• confusion,
• hallucinations,
• severe headache,
• pounding in the neck or ears,
• nosebleed,
• irregular heartbeats,
• nausea,
• vomiting,
• upset stomach,
• constipation,
• fever,
• chills,
• body aches,
• sudden muscle movements,
• increased sweating, and
• swelling in the legs or feet

Serious side effects of Ropinirole include:

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• falling asleep during normal daytime activities (working, talking, eating, or driving),
• drowsiness,
• increased sexual urges,
• unusual urges to gamble,
• extreme drowsiness,
• falling asleep suddenly (even after feeling alert),
• worsening or no improvement in the symptoms,
• lightheadedness,
• unusual changes in mood or behavior,
• tremors,
• twitchinguncontrollable muscle movements,
• hallucinations, and
• confusion

Rare side effects of Ropinirole include:

• none

This is not a complete list of side effects and other serious side effects or health problems may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first

• Ropinirole has severe interactions with no other drugs.
• Ropinirole has serious interactions with at least 26 other drugs.
• Ropinirole has moderate interactions with at least 40 other drugs.
• Ropinirole has minor interactions with the following drugs:
  • bazedoxifene/conjugatedestrogens
  • benazepril
  • conjugated estrogens
  • conjugated estrogens, vaginal
  • estradiol
  • estrogens conjugated synthetic
  • estropipate
  • mestranol

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this drug, tell your doctor or pharmacist of all the drugs you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Contraindications

• Known hypersensitivity/allergic reaction (includingurticaria,angioedema, rash,pruritus) to ropinirole or any of the excipients

Effects of drug abuse

• None

Short-Term Effects

See “What Are Side Effects Associated with Using Ropinirole?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Ropinirole?”

Cautions

• Risk ofsomnolence与使用restless legssyndrome, as well as (rare) risk of晕厥,hypotension, and hallucinations
• May cause psychotic-like behavior; abnormal thinking and behavior can consist of one or more of a variety of manifestations including paranoid ideation, delusions, hallucinations, confusion, disorientation, aggressive behavior, agitation, anddelirium; the risk may be increased in the elderly; consider dose reduction or stopping the medication if a patient develops psychiatric symptoms while taking the medication
• Risk of orthostatic hypotension with the extended-release formulation
• Possible risk of erratic behavior associated withdopamineagonists, compulsive behavior including urge to gamble and increased sexual urges
• Potential for elevation in blood pressure and changes in heart rate should be considered when treating patients withcardiovascular disease与extended-release formulation
• Dyskinesiais seen with concurrent use of levodopa
• Increased risk of melanoma development andpleuralretroperitoneal fibrosis reported, but causation not established; monitoring warranted
• Use caution in patients with a history of hepatic/renal impairment, psychotic disorders, dyskinesias, restless leg syndrome
• In patients with advanced Parkinson’s disease, dyskinesia may occur
• 在开始治疗之前,患者应该广告vised of the potential to develop drowsiness and specifically asked about factors that may increase risks such as concomitantly taking sedating medications or alcohol; the presence of sleep disorders (other than RLS), and concomitant medications that increase ropinirole plasma levels (e.g.,ciprofloxacin); if a patient develops significant daytime sleepiness or episodes of falling asleep during activities that require active participation (e.g., driving a motor vehicle, conversations, eating); therapy should be discontinued; if the decision is made to continue therapy patients should be advised to not drive and avoid other potentially dangerous activities; there is insufficient information to establish whether dose reduction will eliminate episodes of falling asleep while engaged inactivities of daily living
• Patients with Parkinson’s disease may have impaired ability to respond normally to a fall in blood pressure after standing from lying down or seated position; patients receiving therapy should be monitored for signs and symptoms of orthostatic hypotension, especially during dose escalation, and should be informed of the risk for syncope and hypotension

Withdrawal symptoms

• Abrupt withdrawal or significant dosage reduction associated with a syndrome resemblingneurolepticmalignantsyndrome (characterized by elevated temperature,muscularrigidity, altered consciousness, and autonomic instability); see Administration section for how to gradually discontinue the drug
• Symptoms including insomnia, apathy, anxiety, depression, fatigue, sweating, and pain reported during taper or after discontinuation of dopamine agonists; these symptoms generally do not respond to levodopa
• Before discontinuation, patients should be informed about potential withdrawal symptoms, and monitored during and after discontinuation; in case of severe withdrawal symptoms, a trial re-administration of a dopamineagonistat the lowesteffective dosemay be considered

Augmentation and rebound in restless leg syndrome

• Augmentation is a phenomenon in which dopaminergic medication causes a worsening of symptom severity above and beyond the level, at the time the medication was started
• Augmentation symptoms may include earlier onset of symptoms in the evening (or even the afternoon), increase in symptoms, and spread of symptoms to involve other extremities
• Rebound refers to new onset of symptoms in the early morning hour
• Therapy should be reviewed and dosage adjustment or discontinuation of treatment considered with augmentation and early-morning rebound in restless syndrome; when discontinuing therapy in patients with restless leg syndrome, gradual reduction of the daily dose is recommended whenever possible

Pregnancy and Lactation

• There are no adequate data on the developmental risk associated with use in pregnant women; in animal studies, ropinirole had adverse effects on development when administered to pregnant rats at doses similar to (neurobehavioral impairment) or greater than (teratogenicity and embryolethality at over 36 times) maximum recommended human dose (MRHD) for Parkinson’s disease.
• There are no data on the presence of ropinirole in human milk, the effects of ropinirole on the breastfed infant, or effects of ropinirole on milk production; however, inhibition of lactation is expected because ropinirole inhibits the secretion ofprolactinin humans; ropinirole or metabolites, or both, are present in rat milk
• Developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed infant from ropinirole or the underlying maternal condition