rotigotine (Neupro)
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Introduction
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
- 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
- drug adverse effects of adrenergic receptor agonists
- drug adverse effects of dopaminergic receptor agonists
- drug adverse effects of sympathomimetic(s)
Mechanism of action
- dopamine D1 receptor agonist dopamine D2 receptor agonist dopamine D3 receptor agonist Schwarz Pharma
More general terms
References
- ↑ http://www.fda.gov/cder/foi/label/2007/021829lbl.pdf
- ↑ 2.0 2.1 Prescriber's Letter 14(6): 2007 New Drug: Neupro (Rotigotine Transdermal System) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230602&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 3.0 3.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2008/safety08.htm#neupro
- ↑ 4.0 4.1 Prescriber's Letter 19(7): 2012 Neupro Patch (Rotigotine) Update Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=280705&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
- ↑ 6.0 6.1 Medscape: rotigotine (Rx)Neupro http://reference.medscape.com/drug/neupro-rotigotine-343039
- ↑ 7.0 7.1 7.2 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: https://www.ncbi.nlm.nih.gov/pubmed/32667654 Free article https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2768248