Dosing and uses of Neupro (rotigotine)
Adult dosage forms and strengths
transdermal patch
- 1mg/24 hr
- 2mg/24 hr
- 3mg/24 hr
- 4mg/24 hr
- 6mg/24 hr
- 8mg/24 hr
Parkinson Disease
Initial: Apply 2 mg/24 hr transdermal patch qDay for early-stage disease or 4 mg/24 hr for advanced-stage disease
May be increased as needed by increments of 2 mg/24 hr at weekly intervals
Not to exceed 6 mg/24 hr patch qDay for early-stage disease or 8 mg/24 hr for advanced-stage disease
To discontinue treatment, reduce dose gradually (no faster than 2 mg/24 hr every other day) until completely withdrawn
Restless Legs Syndrome
Initial: Apply 1 mg/24 hr transdermal patch qDay
May be increased as needed by increments of 1 mg/24 hr at weekly intervals and as tolerated
Not to exceed 3 mg/24 hr patch qDay
To discontinue treatment, reduce dose gradually (no faster than 1 mg/24 hr every other day) until completely withdrawn
Administration
Apply patch at same time qDay
Apply to clean, dry, intact skin on front of abdomen, high, hip, flank, shoulder, or upper arm
Press the patch firmly to the skin for 30 seconds; check the adherence to the skin, particularly around the edges
Rotate application site each day
Do not apply to the same site more than once every 14 days
Monitor: BP, ophthalmic function
Pediatric dosage forms and strengths
Safety and efficacy not established
Neupro (rotigotine) adverse (side) effects
>10% (Early-stage Parkinson Disease)
Nausea (34-48%)
Application site reactions (including erythema, pruritus, irritation, burning, dermatitis, inflammation, papulae, vesicle, pain) (21-46%)
Dizziness (14-22%)
Somnolence (12-20%)
Vomiting (10-20%)
Fatigue (6-18%)
Insomnia (5-11%)
Hyperhidrosis (3-11%)
1-10% (Advanced-stage Parkinson Disease)
Application site reactions (36-46%)
Somnolence (32%)
Nausea (22-28%)
Dizziness (14-23%)
Dyskinesia (14-17%)
Edema peripheral (9-14%)
Insomnia (9-14%)
Hallucinations (7-14%)
Arthralgia (8-11%)
1-10% (Restless Legs Syndrome)
Application site reactions (23-43%)
Nausea (15-23%)
Headache (15-21%)
Asthenia (7-14%)
1-10% (Early-stage Parkinson Disease)
Abnormal dreams (2-7%)
Erythema (3-6%)
Anorexia (2-6%)
Depression (2-5%)
Edema peripheral (2-4%)
Dyspepsia (2-3%)
EKG, T- ave abnormal (2-3%)
Weight loss (2-3%)
Balance disorder (2-3%)
Tinnitus (2-3%)
Hiccups (2-3%)
Pruritic rash (2-3%)
Erectile dysfunction (2-3%)
Lethargy (1-2%)
Orthostatic hypotension (1-2%)
1-10% (Advanced-stage Parkinson Disease)
Vomiting (8-10%)
Headache (8-10%)
Constipation (5-9%)
Diarrhea (5-7%)
Hypertension (3-5%)
Nightmares (3-5%)
Paraesthesias/Dysesthesias (3-4%)
Tremor (3-4%)
Asthenia (3-4%)
Cough (3%)
Nasal Congestion (3%)
Sinus congestion (2-3%)
Erythema (2-3%)
Hyperhidrosis (1-3%)
Musculoskeletal pain (2%)
1-10% (Restless Legs Syndrome)
Nasopharyngitis (5-10%)
Somnolence (5-10%)
Insomnia (2-10%)
Dizziness (5-9%)
Pruritus (3-9%)
Xerostomia (3-7%)
Constipation (2-6%)
Hyperhidrosis (1-5%)
Vomiting (2-4%)
Muscle spasms (1-4%)
Hypertension (1-4%)
Hot flushes (1-4%)
Dyspepsia (1-3%)
Vertigo (1-3%)
Sinusitis (1-3%)
Abnormal dreams (1-3%)
Sleep attacks (1-2%)
Erythema (1-2%)
Warnings
Contraindications
Hypersensitivity
Cautions
May cause sudden onset of sleep while engaging in activities of daily living, compulsive disorders (eg, pathologic gambling, hypersexuality, increased libido, repetitive meaningless actions), hallucinations, and psychotic-like behavior
Contains sodium metabisulfite that may cause allergic-type reactions Somnolence is common; falling asleep during activities of daily living observed
May cause symptomatic hypotension and syncope
May increase blood pressure and heart rate
Dose dependent increases in weight and fluid retention observed
May potentiate dopaminergic side effects of levodopa and cause or exacerbate dyskinesia
Avoid abrupt withdrawal; symptoms resembling neuroleptic malignant syndrome (characterized by elevated temperature, muscular rigidity, altered consciousness, rhabdomyolysis, and/or autonomic instability) with no other obvious etiology, has been reported in association with rapid dose reduction
Application site reactions are frequent and dose related
Restless leg syndrome rebound/augmentation may occur as dose wears off
Remove patch before MRI; backing layer of patch contains aluminum
Heat may increase absorption; avoid exposure to external heat sources (eg, heating pads, electric blankets, sauna)
Fibrotic complication reported (eg, retroperitoneal fibrosis, pleural effusion, pericarditis)
Binding to melanin-pigmented tissues reported
Hallucinations/psychotic -like behavior and dyskinesia may occur
Monitor for melanoma; increased risk reported for patients receiving therapy
Pregnancy and lactation
Pregnancy category: C
Lactation: not known if excreted in breast milk; discontinue drug or do not nurse (may inhibit lactation)
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Neupro (rotigotine)
Mechanism of action
Non-ergolinic D3/D2/D1 dopamine agonist
Effective in treating Parkinson disease by stimulating D2 receptors within the caudate-putamen in the brain
The precise mechanism of action for treating restless legs syndrome is unknown; thought to be related dopamine receptor stimulation
Absorption
Bioavailability: 37%
Peak plasma time: 15-18 hr
Release rate: 45% in 24 hr (0.2 mg/sq.cm/24 hr)
Distribution
Protein Bound: 92% (in vitro); 89.5% (in vivo)
Vd: 84 L/kg
Metabolism
Metabolized by N-dealkylation and direct/secondary conjugation
Elimination
Half-life, biphasic: 3 hr (initial); 5-7 hr (terminal)
Excretion: 71% urine; 23% feces
