Requip 2 mg Tablets

Brand Name

This pharmaceutical agent is marketed under the trade name Requip, a label widely utilized in the management of neurological conditions.

International Non-Proprietary Name

The active substance is identified globally as ropinirole, adhering to the standardized nomenclature for medicinal compounds.

Form of Release

The drug is available in two oral formulations to suit varying patient requirements. It comes as immediate-release tablets in strengths of 0.25 milligrams, 0.5 milligrams, 1 milligram, 2 milligrams, 3 milligrams, 4 milligrams, and 5 milligrams. An extended-release tablet version is offered in doses of 2 milligrams, 4 milligrams, 6 milligrams, 8 milligrams, and 12 milligrams, designed for once-daily use.

Composition

The primary ingredient is ropinirole hydrochloride, which delivers its therapeutic effects through receptor activation. Immediate-release tablets include excipients such as lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate to ensure stability and disintegration. Extended-release tablets incorporate a controlled-release matrix with hypromellose, alongside additional components like mannitol and glyceryl behenate, facilitating a steady release profile.

Pharmacologic Properties

Pharmacodynamics

This medication functions as a non-ergot dopamine agonist, selectively stimulating D2 and D3 dopamine receptors in the brain. By mimicking dopamine’s action, it compensates for the neurotransmitter shortfall observed in specific disorders, particularly within the basal ganglia, a key area for motor regulation. Its preference for D2 receptors enhances motor control, while D3 activity may influence mood and sensory responses, offering a broad therapeutic scope.

Clinical studies highlight its effectiveness in reducing motor symptoms like rigidity and tremors, alongside alleviating sensory disturbances. The mechanism focuses on symptom management by enhancing dopaminergic signaling, without modifying the underlying disease course. Its receptor specificity minimizes off-target effects, providing a balanced approach to treatment.

Pharmacokinetics

Upon oral administration, the medication absorbs rapidly from the gastrointestinal tract, reaching peak plasma concentrations in 1 to 2 hours for immediate-release forms and 6 to 10 hours for extended-release versions. Food, especially high-fat meals, may delay absorption but does not significantly reduce bioavailability, which averages around 55 percent due to first-pass metabolism.

The substance distributes widely, with a volume of distribution of approximately 7 liters per kilogram, indicating good tissue penetration, including the central nervous system. It binds to plasma proteins at about 40 percent, leaving a substantial portion free to act. Metabolism occurs primarily in the liver via cytochrome P450 enzyme CYP1A2, producing inactive metabolites like carboxylic acid derivatives. The half-life is around 6 hours for immediate-release and up to 8 hours for extended-release, influenced by hepatic function.

Excretion happens mainly through urine, with over 88 percent eliminated as metabolites and less than 10 percent unchanged. Renal clearance plays a minor role, as the drug is extensively metabolized before elimination. A small fraction exits via feces, but the hepatic route dominates its clearance profile.

Indications for Use

Conditions and Disorders

The medication is prescribed for Parkinson’s disease, a progressive disorder marked by dopamine depletion in the brain. It manages early-stage symptoms such as tremors, stiffness, and slowed movement as a standalone therapy, and in later stages, it supports levodopa to minimize motor fluctuations. It is also indicated for moderate to severe restless legs syndrome, reducing the urge to move and associated discomfort during rest.

Requip provides consistent relief for these conditions, enhancing mobility and sleep quality. Its dual role reflects its adaptability in addressing dopamine-related challenges, though its primary use remains focused on these approved indications, with limited evidence for broader applications.

Contraindications

Conditions Prohibiting Use

The drug is contraindicated in patients with hypersensitivity to ropinirole or its components, as reactions could range from mild rashes to severe allergic responses. Severe hepatic impairment restricts its use, given its extensive metabolism in the liver, which could lead to accumulation and toxicity.

It should not be used in individuals with a history of psychosis or uncontrolled impulse control disorders, as dopaminergic stimulation may worsen these states. Significant cardiovascular conditions, such as severe hypotension or recent cardiac events, also preclude administration due to potential blood pressure effects.

Method of Administration and Dosage

Administration Guidelines

The medication is taken orally, with immediate-release tablets typically administered three times daily and extended-release tablets once daily, preferably in the morning. It can be taken with or without food, though meals may reduce nausea if consumed alongside. Tablets should be swallowed whole with water, avoiding breaking or chewing, especially for extended-release forms.

Dosage for Adults and Children

For adults with Parkinson’s, immediate-release therapy starts at 0.25 milligrams three times daily, increasing weekly by 0.25 milligrams per dose to a usual range of 3 to 24 milligrams daily. Extended-release begins at 2 milligrams daily, escalating by 2 milligrams weekly to a maximum of 24 milligrams. For restless legs syndrome, immediate-release dosing is 0.25 milligrams once daily, 1 to 3 hours before bedtime, titrating to 4 milligrams if needed. Pediatric use is not approved, as safety and efficacy in children remain unstudied.

Dose Adjustments for Specific Conditions

In mild to moderate renal impairment (creatinine clearance 30 to 50 milliliters per minute), standard dosing is typically safe, but severe impairment (below 30 milliliters per minute) may require cautious titration. Moderate to severe hepatic impairment necessitates lower doses or avoidance, as metabolism is significantly affected. Adjustments should align with clinical monitoring and patient response.

Side Effects

Potential Adverse Reactions

Common effects include nausea, dizziness, and fatigue, often tied to dopaminergic stimulation and most noticeable during initial use or dose increases. Drowsiness, headache, and leg swelling may also occur, generally subsiding with continued therapy. Some patients experience orthostatic hypotension, leading to lightheadedness upon standing.

Less frequent reactions involve hallucinations, confusion, or compulsive behaviors like excessive spending, particularly at higher doses or in predisposed individuals. Rarely, sudden sleep onset or worsening motor symptoms emerge, requiring prompt medical attention. Severe behavioral shifts or allergic responses necessitate urgent evaluation.

Overdose

Symptoms of Excessive Intake

Overdosing may cause agitation, confusion, and low blood pressure, reflecting excessive dopamine activity. Severe cases can lead to hallucinations, rapid heart rate, or loss of consciousness, with respiratory irregularities posing significant risks. Symptoms vary based on the amount ingested and individual tolerance.

First Aid Measures

Stop the drug and seek emergency care immediately. Activated charcoal may reduce absorption if administered within an hour, provided the patient is alert. No specific antidote exists, so treatment focuses on supportive care, such as stabilizing blood pressure and monitoring vitals. Professional oversight is critical to manage severe effects.

Drug Interactions

Effects on Other Medications

The medication can enhance the effects of other dopaminergic agents, like levodopa, increasing risks of dyskinesia or hypotension. It may reduce the efficacy of dopamine antagonists, such as antipsychotics, by counteracting their action. CYP1A2 inhibitors, like ciprofloxacin, could raise its levels, while inducers, like smoking, might lower its potency.

Requip may amplify sedation with central nervous system depressants, such as alcohol or benzodiazepines, heightening drowsiness risks. Caution is advised with drugs affecting blood pressure, like antihypertensives, due to potential additive effects on circulation.

Compatibility with Alcohol and Food

Alcohol may intensify drowsiness or dizziness, so limited intake is recommended to avoid excessive sedation. Food can delay absorption slightly but may ease nausea, offering a practical administration option. No specific dietary restrictions apply beyond general caution with high-fat meals.

Special Precautions

Use During Pregnancy and Breastfeeding

Limited data exist on pregnancy use, with no definitive human evidence of safety or risk. Animal studies suggest potential fetal effects, so the drug should only be used if benefits outweigh uncertainties, under medical supervision. It may pass into breast milk, so nursing mothers should consult a physician, possibly suspending lactation during therapy.

Impact on Driving and Machinery Operation

The medication may cause drowsiness, sudden sleep episodes, or dizziness, particularly early in treatment or at higher doses. Patients should evaluate their response before driving or operating machinery, avoiding these tasks if affected. Caregivers may need to monitor those at risk of abrupt sleep onset.

Considerations for Elderly and Pediatric Patients

Elderly patients generally tolerate it well, though reduced hepatic or renal function may require dose adjustments in moderate to severe cases. Requip is not approved for children, as its role in pediatric conditions lacks evidence, restricting use to adults.