Lopinirole is a dopamine receptor agonist primarily used to treat Parkinson's disease and Restless Legs Syndrome (RLS). This medication stimulates dopamine receptors in the brain, improving motor dysfunction and limb discomfort symptoms. In Parkinson's treatment, it is often combined with levodopa-based medications to delay the wearing-off phenomenon.
For RLS patients, it significantly reduces involuntary limb movements and abnormal sensations, improving sleep quality. The drug's effects can last up to 12 hours, and dosage adjustments should be made under medical supervision.
The main brand name is Requip®, and the generic drug is Lopinirole. Different pharmaceutical manufacturers may have different brand names, but the active ingredient is all lopinirole hydrochloride. The medication comes in immediate-release tablets and extended-release capsules, which should be selected based on patient age and severity of symptoms.
Lopinirole belongs to Dopamine D2/D3 receptor agonists, classified pharmacologically as a dopaminergic agent. Its mechanism of action differs from traditional dopamine precursors, directly stimulating specific neural receptors to improve symptoms.
The primary indications include: 1. Motor symptoms of Parkinson's disease, especially as an adjunct for the "wearing-off" and "on-off" phenomena; 2. Moderate to severe Restless Legs Syndrome, when non-pharmacological treatments are ineffective.
In Taiwan, this medication requires a prescription from a neurologist or internist and should not be self-adjusted. Patients over 65 should pay special attention to dosage adjustments to avoid side effects.
Contraindications include severe heart disease, uncontrolled glaucoma, and hypersensitivity to the ingredients. Pregnancy is classified as Category C; risks should be carefully evaluated during pregnancy and breastfeeding. Avoid riding motorcycles or operating machinery within 6 hours of taking the medication.
Concurrent use with MAO inhibitors may induce involuntary movements, and concomitant use with antipsychotics may reduce efficacy. If patients develop uncontrollable behaviors such as gambling or binge eating during treatment, medication should be discontinued immediately and medical advice sought.
When combined with levodopa, monitor for abnormal movements or hypotension. Use with antihistamines may increase sedation. Monoamine oxidase inhibitors may trigger hypertensive crises.
Certain antiarrhythmic drugs (e.g., quinidine) can increase lopinirole blood levels, raising cardiac toxicity risk. Herbal supplements like St. John’s Wort may reduce efficacy; avoid self-medication during treatment.
The starting dose for Parkinson's disease is 0.25 mg daily, gradually increasing every 3 to 7 days to the target dose. For RLS, treatment typically begins with 0.5 mg taken at bedtime, with a maximum dose not exceeding 0.5 mg per day. Extended-release formulations should be swallowed whole; do not crush or chew.
Evaluate efficacy and side effects every 3 to 6 months during treatment. Patients over 65 or with liver impairment should have reduced doses to prevent excessive sedation and falls.
If a dose is missed and the next dose is close, skip the missed dose and take the next as scheduled. Do not double doses to make up for missed ones, as this may cause adverse effects from high doses. Use reminders or pillboxes to prevent missed doses.
Symptoms of overdose include severe drowsiness, muscle rigidity, and altered consciousness. Seek immediate medical attention and bring the medication container for reference. Emergency treatments may include gastric lavage, administration of antagonists, or supportive care.
If respiratory depression or coma occurs, call 119 immediately and specify the medication name and dose. Store medications out of reach of children in a secure place.
Lopinirole can be taken with or without food, but it is recommended to take it at a fixed time to maintain stable drug levels. Taking it with meals may reduce the absorption rate, but the total absorption remains largely unchanged. Patients are advised to choose a consistent time (such as before bed or after waking) and avoid high-fat meals to reduce gastrointestinal discomfort.
How should I handle visual or auditory hallucinations caused by long-term Lopinirole use?About 5-10% of patients may experience mild, harmless visual or auditory hallucinations. If these symptoms interfere with daily life, consult a doctor to adjust the dose. Keep the sleeping environment well-lit to reduce hallucinations in dark areas, and have regular follow-ups to assess medication safety. Avoid driving or operating machinery alone.
Does combining Lopinirole with anxiolytics or sleeping pills increase drowsiness?Yes, combining with benzodiazepines (e.g., diazepam) or sedative antihistamines may enhance daytime sleepiness. Doctors may recommend reducing the dose of one or adjusting the timing (e.g., taking sleeping pills at bedtime). If excessive fatigue occurs, avoid operating vehicles.
How can I prevent orthostatic hypotension caused by Lopinirole in daily life?Move slowly when standing, sit for a few minutes before walking after getting up. Maintain adequate hydration and avoid dehydration. Wearing compression stockings can help blood circulation. If dizziness occurs, sit down and elevate the legs; seek medical advice for dose adjustment if severe. Avoid hot baths or hot springs to reduce blood pressure drops.
What should I do if I suddenly stop Lopinirole to avoid withdrawal symptoms?Sudden discontinuation may cause nausea, anxiety, or Parkinsonian rebound symptoms. Tapering off gradually is recommended, typically reducing the dose by 25-50% weekly over several weeks to months. A personalized plan should be developed by a physician based on disease severity and history. Do not stop medication abruptly without medical guidance to prevent worsening of symptoms.
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