Neupro
Neupro
Generic Name
Neupro
Brand Names
for *rotigotine*, a non‑ergot dopamine‑agonist administered via a transdermal patch. It is primarily indicated for the management of Parkinson’s disease (PD) and rest‑less legs syndrome (RLS).
Mechanism
- Partial dopamine agonist
- Selectively stimulates D₂, D₃, and D₄ dopamine receptors with high affinity, mimicking dopamine actions in basal ganglia circuits.
- Sustained release
- Continuous dermal delivery maintains steady plasma levels, avoiding the pulsatile dopaminergic stimulation associated with oral levodopa, thereby reducing motor fluctuations and dyskinesia.
- Neuroprotective potential
- Preclinical data suggest rotigotine may modulate α‑synuclein aggregation and reduce oxidative stress, although clinical benefit remains investigational.
Pharmacokinetics
| Parameter | Key Findings |
| Absorption | Dermal absorption yields a C_max of ~0.1 µg/mL by 6 h, with ~2.4 µg/mL at steady state (≈48 h). |
| Half‑life | ~3-5 h (but patch release extends effective half‑life). |
| Bioavailability | 18–23 % relative to oral dosing (patch bypasses first‑pass metabolism). |
| Metabolism | Hepatic via CYP2D6 and CYP3A4; metabolites inactive. |
| Excretion | Primarily renal (≈60 %) and fecal. |
| Steady state | Achieved in ~5–7 days; patch replacement every 1–2 days (typically 3–5 µg/h → 5–7 µg/h patches). |
Indications
- Parkinson’s Disease
- *Off‑time* therapy for motor fluctuations in patients receiving and/or unable to tolerate levodopa.
- Adjunct to levodopa for early‑stage PD (controlled by the FDA).
- Rest‑less Legs Syndrome (approved in some countries, off‑label in others).
- Compulsive sexual behaviour (investigational; not FDA approved).
Contraindications
- Contraindications
- Known hypersensitivity to rotigotine or patch components.
- Severe hepatic dysfunction (CR ≥3).
- Warnings
- Fluid retention / edema – monitor weight and signs of heart failure.
- Psychiatric – risk of impulse control disorders, hallucinations, and mood changes.
- Cardiogenic – potential bradycardia, hypotension, or syncope; avoid in severe cardiac disease or uncontrolled hypertension.
- Precautions
- Use with caution in patients with skin disorders (eczema, dermatitis) or scar tissue.
- Avoid exposure to high temperatures (>38 °C) which can increase systemic levels.
Dosing
| Stage | Patch Strength | Duration | Replacement Frequency | Dosing Notes |
| Initiation | 2 µg/h | 24 h | Every 3–5 days (per product labeling) | Start at 2 µg/h; titrate upward by 2 µg/h increments weekly. |
| Maintenance | 4–7 µg/h | 24 h | Every 4–5 days | Adjust based on motor control & tolerability. |
• Patch Placement: Rotate sites (abdomen, flank, upper arm, thigh) to avoid skin irritation.
• Patch Removal: If adverse cutaneous reaction occurs, remove patch and reapply at a different site with a temporary skin barrier.
Adverse Effects
Common (≥10 % incidence)
• Nausea, vomiting
• Somnolence, dizziness
• Dysphagia
• Abdominal pain, constipation
Serious (≤1 % incidence)
• Impulse control disorders (punding, gambling, hypersexuality) – warrants patient education & monitoring.
• Psychosis / hallucinations – assess baseline neuropsychiatric status.
• Fluid retention with heart failure – monitor vitals, creatinine.
• Hypotension – especially upon patch removal or high‑dose titration.
Monitoring
- Clinical: Regular assessment of motor scores (UPDRS Part III), daytime sleepiness, and impulse control behaviors.
- Vital signs: Blood pressure (supine and standing) and heart rate weekly during titration.
- Signs of fluid overload: Weight, peripheral edema.
- Skin changes: Inspect patch site daily for dermatitis or contact reactions.
- Laboratory: Liver function tests quarterly; renal panel as clinically indicated.
Clinical Pearls
- Avoid heat: The patch’s absorption increases at temperatures above 38 °C; instruct patients to limit sunbathing or hot tubs.
- Patch‑Hematologic partner: For patients concurrently on anticoagulants, skin reactions can lead to local microvascular changes; monitor for petechiae or bruising.
- “On‑off” transitions: Rapid removal of the patch can precipitate a sudden “off” state; if patients feel tremor resurgence within 75 yrs) tolerate lower basal doses (2 µg/h) and may benefit from slower titration due to altered pharmacokinetics.
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• *This drug card is for educational purposes and reflects the latest FDA‑approved indications and clinical data. Always consult current prescribing information and institutional guidelines when initiating therapy.*