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rotigotine (Neupro)
RECALL April 9, 2008 [3]; REFROMULATED July 2012 [4]
- due to formation of rotigotine crystals in the patches
- when the drug crystallizes, less drug is available to be absorbed through the skin & the efficacy of the product may vary
- reformulated July 2012; re-introduced to the market[4]
Indications:
- early Parkinson's disease
- restless legs syndrome
- may improve frontal lobe function & activities of daily living in patients with mild-moderate Alzheimer's disease [7]
* does not affect global cognition in Alzheimer's disease [7]
Dosage:
- transdermal patch 1, 2, 4, & 6 mg/24 hours (Neupro)*
- rotate from day to day (abdomen, thigh, hip, flank, shoulder, or upper arm)
- no changes needed for geriatric dosing
- Parkinson's disease
- start 2 mg/24 hours, lowest effective dose 4 mg/24 hours [2]
- restless legs syndrome
- start 1 mg/24 hours; max 3 mg/24 hours [6]
No dosage adjustment with renal insufficiency
Pharmacokinetics:
- steady-state plasma concentrations within 2-3 days
- volume of distribution 84 L/kg
- protein binding 90%
- extensively metabolized by conjugation & N-dealkylation
- biphasic elimination
- initial 1/2life of 3 hours
- terminal 1/2life of 5-7 hours
- primarily eliminated in the urine as inactive conjugates
Adverse effects:
- dizziness
- nausea
- drowsiness
- somnolence
- sudden onset of sleep (sleep attack)
- insomnia
- postural hypotension
- hallucinations
- syncope ?
- increased heart rate 2-4 beats/min
- weight gain 2%
- may potentiate diskinesias
- application site reactions
Mechanism of action:
- dopamine D1 receptor agonist dopamine D2 receptor agonist dopamine D3 receptor agonist Schwarz Pharma
Interactions
drug adverse effects (more general classes)
General
dopaminergic receptor agonist
pharmacologic agents for treatment of Parkinson's disease
Properties
AGONIST-FOR: adrenergic receptor
References
- http://www.fda.gov/cder/foi/label/2007/021829lbl.pdf
- Prescriber's Letter 14(6): 2007
New Drug: Neupro (Rotigotine Transdermal System)
Detail-Document#: 230602
(subscription needed) http://www.prescribersletter.com
- FDA MedWatch
http://www.fda.gov/medwatch/safety/2008/safety08.htm#neupro
- Prescriber's Letter 19(7): 2012
Neupro Patch (Rotigotine) Update
Detail-Document#: 280705
(subscription needed) http://www.prescribersletter.com
- Medical Knowledge Self Assessment Program (MKSAP) 17,
American College of Physicians, Philadelphia 2015
- Medscape: rotigotine (Rx)Neupro
http://reference.medscape.com/drug/neupro-rotigotine-343039
- Koch G et al
Effect of Rotigotine vs Placebo on Cognitive Functions Among
Patients With Mild to Moderate Alzheimer DiseaseA Randomized Clinical Trial.
JAMA Netw Open. 2020;3(7):e2010372
PMID: 32667654 Free article
https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2768248