may [18:<30 mL/min) not receiving dialysis. 1 17 Moderate hepatic impairment: No relevant changes in plasma concentrations. 1 Severe hepatic impairment: Not studied. 1 Geriatric patients: Plasma concentrations in healthy individuals and patients 65 80 years of age similar to those in younger adults. 1 20 Exposure in geriatric patients> 80 years of age not studied, but may be higher due to skin changes with aging. 1 Distribution Extent Distributes into milk in rats; not known whether the drug and/or its metabolites distribute into human milk. 1 Plasma Protein Binding Approximately 92% to human plasma proteins in vitro; 89.5% in vivo. 1 Elimination Metabolism Extensively metabolized by conjugation and N -dealkylation. 1 16 Major metabolites in urine include rotigotine sulfate, rotigotine glucuronide, N -despropyl-rotigotine sulfate, and N -desthienylethyl-rotigotine sulfate. 1 16 Elimination Route Approximately 71 and 23% of a single IV dose excreted in urine and feces, respectively, as metabolites; less than 1% excreted as unchanged drug in urine. 1 16 Half-life Biphasic (after removal of patch); initial half-life of 3 hours and terminal half-life of 5 7 hours. 1 Actions Exhibits binding specificity for and intrinsic activity at dopamine D 1 , D 2 , D 3 , D 4 , and D 5 receptors, with highest affinity for D 3 subtype. 15 23 Demonstrates antagonistic effects at α 2B -adrenergic receptors and agonistic effects at serotonin type 1A (5-hydroxytryptamine [5-HT 1A ]) receptors, but no activity on 5-HT 2B receptors. 15 23 Parkinsonian syndrome: Mechanism of action not fully elucidated. 1 Appears to act by stimulating dopamine receptors (D 3 , D 2 , and D 1 ) in the caudate putamen of the brain. 1 23 Restless legs syndrome: Precise mechanism of action unknown; appears to be related to ability to stimulate dopamine receptors. 1 23 Advice to Patients Importance of reading the manufacturer's patient information before beginning transdermal rotigotine therapy and each time the drug is dispensed. 1 Importance of using the rotigotine transdermal system (patch) as prescribed. 1 Importance of instructing patients to wear system continuously for 24 hours, then to remove the patch and immediately apply a new one. 1 If a patient forgets to change a patch, they should be advised to apply a new patch as soon as possible and then replace it at the usual time the following day. 1 Risk of severe allergic reactions, including allergic-type reactions in patients with sulfite sensitivity. 1 Importance of advising patients to immediately remove the patch and seek immediate medical attention if they experience swelling of the lips or tongue, chest pain, and/or difficulty breathing or swallowing. 1 Importance of advising and alerting patients of the potential for sedating effects, including somnolence and particularly the possibility of falling asleep without feeling drowsy or without warning while engaged in activities of daily living. 1 Patients should avoid driving or engaging in other potentially dangerous activities until effects on the individual are known. 1 Importance of informing patients that hallucinations or other psychotic-like behavior can occur during therapy, particularly in geriatric patients with parkinsonian syndrome. 1 Risk of symptomatic (e.g., dizziness, nausea, sweating) or asymptomatic orthostatic hypotension and syncope during therapy, particularly during initial therapy and following an increase in dosage. 1 Advise patients to avoid rising rapidly after sitting or lying down, especially if they have been in a seated or recumbent position for prolonged periods and/or if they are just beginning transdermal rotigotine therapy. 1 Advise patients to contact their clinician if they experience any signs or symptoms of lowered BP during therapy. 1 Risk of increased BP or exacerbation of hypertension and increased heart rate. 1 Importance of asking patients whether they have developed any new or increased urges or compulsive behaviors (e.g., gambling urges, sexual urges, uncontrolled spending, binge eating) while receiving transdermal rotigotine and of advising them of the importance of reporting such urges. 1 21 Risk of weight gain and fluid retention, which may manifest as peripheral edema. 1 Patients should contact their clinician if they experience swelling or fluid retention, especially in the ankles or legs, or have an unusually fast increase in weight. 1 Risk of new onset or exacerbation of dyskinesia. 1 Importance of informing patients that application site reactions can occur with transdermal rotigotine and that the application site should be rotated on a daily basis. 1 The patch should not be applied to the same application site more often than once every 14 days. 1 Patients should report persistent application site reactions (lasting more than a few days), increases in severity, or skin reactions that spread outside the application site. 1 If there is a skin rash or irritation from the transdermal system, direct sunlight on the area should be avoided until the skin heals; such exposure may lead to changes in skin color. 1 Importance of advising patients with parkinsonian syndrome that they are at higher risk of developing melanoma. 1 Advise patients to monitor for melanoma frequently and on a regular basis when using transdermal rotigotine for any indication. 1 Importance of informing patients that transdermal rotigotine may cause restless legs symptoms to have an earlier onset during the day or become worse. 1 Importance of informing patients to remove the rotigotine patch before undergoing MRI or cardioversion to avoid possible skin burns. 1 Importance of advising patients about the potential for heat application to increase rotigotine absorption from the patch. 1 Instruct patients to avoid applying external heat sources to the transdermal system and to avoid direct sun exposure of the transdermal system. 1 Importance of informing patients that transdermal rotigotine may cause nausea, vomiting, and general GI distress (i.e., dyspepsia, abdominal discomfort). Importance of following recommended procedure for administration, removal, and disposal of rotigotine transdermal systems and of reviewing the instruction sheet provided by the manufacturer. 1 Importance of patient (or individual assisting the patient) thoroughly washing hands with soap and water after handling the rotigotine transdermal system (e.g., initial application, removal) and to wash the application site thoroughly after removing the system. 1 Importance of proper transdermal system disposal, including keeping it out of the reach of children or pets. 1 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription (e.g., CNS depressants including sedatives, antidepressants, and antipsychotics) and OTC drugs and herbal supplements, as well as any concomitant illnesses. 1 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 1 Importance of informing patients of other important precautionary information. 1 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Rotigotine Routes Dosage Forms Strengths Brand Names Manufacturer Topical Transdermal System 1 mg/24 hours (2.25 mg/5 cm 2 ) Neupro UCB 2 mg/24 hours (4.5 mg/10 cm 2 ) Neupro UCB 3 mg/24 hours (6.75 mg/15 cm 2 ) Neupro UCB 4 mg/24 hours (9 mg/20 cm 2 ) Neupro UCB 6 mg/24 hours (13.5 mg/30 cm 2 ) Neupro UCB 8 mg/24 hours (18 mg/40 cm 2 ) Neupro UCB AHFS DI Essentials. Copyright 2017, Selected Revisions March 31, 2014. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. UCB, Inc. Neupro (rotigotine transdermal system) prescribing information. Smyrna, GA; 2012 Apr. 2. Parkinson Study Group. A controlled trial of rotigotine monotherapy in early Parkinson's disease. Arch Neurol . 2003; 60:1721-8. [PubMed 14676046] 3. Watts RL, Jankovic J, Waters C et al. Randomized, blind, controlled trial of transdermal rotigotine in early Parkinson disease. Neurology . 2007; 68:272-6. [PubMed 17202432] 4. Giladi N, Boroojerdi B, Korczyn AD et al. Rotigotine transdermal patch in early Parkinson's disease: a randomized, double-blind, controlled study versus placebo and ropinirole. Mov Disord . 2007; 22:2398-404. [PubMed 17935234] 5. Trenkwalder C, Kies B, Rudzinska M et al. Rotigotine effects on early morning motor function and sleep in Parkinson's disease: a double-blind, randomized, placebo-controlled study (RECOVER). Mov Disord . 2011; 26:90-9. [PubMed 21322021] 6. Poewe WH, Rascol O, Quinn N et al. Efficacy of pramipexole and transdermal rotigotine in advanced Parkinson's disease: a double-blind, double-dummy, randomised controlled trial. Lancet Neurol . 2007; 6:513-20. [PubMed 17509486] 7. LeWitt PA, Lyons KE, Pahwa R et al. Advanced Parkinson disease treated with rotigotine transdermal system: PREFER Study. Neurology . 2007; 68:1262-7. [PubMed 17438216] 8. Trenkwalder C, Benes H, Poewe W et al. Efficacy of rotigotine for treatment of moderate-to-severe restless legs syndrome: a randomised, double-blind, placebo-controlled trial. Lancet Neurol . 2008; 7:595-604. [PubMed 18515185] 9. Hening WA, Allen RP, Ondo WG et al. Rotigotine improves restless legs syndrome: a 6-month randomized, double-blind, placebo-controlled trial in the United States. Mov Disord . 2010; 25:1675-83. [PubMed 20629075] 10. Oertel WH, Benes H, Garcia-Borreguero D et al. Efficacy of rotigotine transdermal system in severe restless legs syndrome: a randomized, double-blind, placebo-controlled, six-week dose-finding trial in Europe. Sleep Med . 2008; 9:228-39. [PubMed 17553743] 11. Oertel WH, Benes H, Garcia-Borreguero D et al. Rotigotine transdermal patch in moderate to severe idiopathic restless legs syndrome: a randomized, placebo-controlled polysomnographic study. Sleep Med . 2010; 11:848-56. [PubMed 20813583] 12. Oertel W, Trenkwalder C, Benes H et al. Long-term safety and efficacy of rotigotine transdermal patch for moderate-to-severe idiopathic restless legs syndrome: a 5-year open-label extension study. Lancet Neurol . 2011; 10:710-20. [PubMed 21705273] 13. Elmer LW, Surmann E, Boroojerdi B et al. Long-term safety and tolerability of rotigotine transdermal system in patients with early-stage idiopathic Parkinson's disease: a prospective, open-label extension study. Parkinsonism Relat Disord . 2012; 18:488-93. [PubMed 22326237] 14. Jankovic J, Watts RL, Martin W et al. Transdermal rotigotine: double-blind, placebo-controlled trial in Parkinson disease. Arch Neurol . 2007; 64:676-82. [PubMed 17502466] 15. Scheller D, Ullmer C, Berkels R et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol . 2009; 379:73-86. [PubMed 18704368] 16. Cawello W, Braun M, Boekens H. Absorption, disposition, metabolic fate, and elimination of the dopamine agonist rotigotine in man: administration by intravenous infusion or transdermal delivery. Drug Metab Dispos . 2009; 37:2055-60. [PubMed 19608695] 17. Cawello W, Ahrweiler S, Sulowicz W et al. Single dose pharmacokinetics of the transdermal rotigotine patch in patients with impaired renal function. Br J Clin Pharmacol . 2012; 73:46-54. [PubMed 21707699] 18. Sprenger FS, Seppi K, Poewe W. Drug safety evaluation of rotigotine. Expert Opin Drug Saf . 2012; 11:503-12. [PubMed 22468676] 19. Benes; H, García-Borreguero D, Ferini-Strambi L et al. Augmentation in the treatment of restless legs syndrome with transdermal rotigotine. Sleep Med . 2012; 13:589-97. [PubMed 22503658] 20. Elshoff JP, Braun M, Andreas JO et al. Steady-state plasma concentration profile of transdermal rotigotine: an integrated analysis of three, open-label, randomized, phase I multiple dose studies. Clin Ther . 2012; 34:966-78. [PubMed 22401642] 21. Schreglmann SR, Gantenbein AR, Eisele G et al. Transdermal rotigotine causes impulse control disorders in patients with restless legs syndrome. Parkinsonism Relat Disord . 2012; 18:207-9. [PubMed 22030321] 22. Braun M, Elshoff JP, Andreas JO et al. Influence of transdermal rotigotine on ovulation suppression by a combined oral contraceptive. Br J Clin Pharmacol . 2009; 68:386-94. [PubMed 19740396] 23. UCB Manufacturing Ireland Ltd. Neupro 1 mg/24 h transdermal patch summary of product characteristics. Shannon, Ireland; 2011 Feb 17. 24. Zanettini R, Antonini A, Gatto G et al. Valvular heart disease and the use of dopamine agonists for Parkinson's disease. N Engl J Med . 2007; 356:39-46. [PubMed 17202454] 25. Andersohn F, Garbe E. Cardiac and noncardiac fibrotic reactions caused by ergot- and nonergot-derived dopamine agonists. Mov Disord . 2009; 15:129-33. 26. US Food and Drug Administration. Sulfites in foods and drugs. FDA Drug Bull . 1983; 13:12. [PubMed 6604672] 27. Sogn D. The ubiquitous sulfites. JAMA . 1984; 251:2986-7. [PubMed 6716628] 28. Koepke JW, Christopher KL, Chai H et al. Dose dependent bronchospasm from sulfites in isoetharine. JAMA . 1984; 251:2982-3. [PubMed 6716626] 29. Twarog FJ, Leung DYM. Anaphylaxis to a component of isoetharine (sodium bisulfite). JAMA . 1982; 248:2030-1. [PubMed 7120631] 30. Baker GJ, Collett P, Allen DH. Bronchospasm induced by metabisulphite containing foods and drugs. Med J Austr . 1981; 2:614-7. 31. Koepke JW, Selner JC, Dunhill AL. Presence of sulfur dioxide in commonly used bronchodilator solutions. J Allergy Clin Immunol . 1983; 72:504-8. [PubMed 6630799] 32. US Food and Drug Administration. Sulfiting agents: labeling in drugs for human use: warning statement. [Docket No. 84N-0113]. Fed Regist . 1985; 50:47558-63. 33. US Food and Drug Administration Center for Food Safety and Applied Nutrition. The reexamination of the GRAS status of sulfiting agents, January 1985. (Doc. No. 223-83-2020.) Bethesda, MD: FASEB Life Sciences Research Office. 34. Braun M, Cawello W, Andreas JO et al. Lack of pharmacokinetic interactions between transdermal rotigotine and oral levodopa/carbidopa. J Clin Pharmacol . 2009; 49:1047-55. [PubMed 19628729] 35. Gamaldo CE, Earley CJ. Restless legs syndrome: a clinical update. Chest . 2006; 130:1596-604. [PubMed 17099042] 36. Earley CJ. Restless legs syndrome. N Engl J Med . 2003; 348:2103-9. [PubMed 12761367] 37. Leschziner G, Gringas P. Restless legs syndrome. Br Med J . 2012; 344:e3056. Next Interactions Print this page Add to My Med List More about rotigotine Side Effects During Pregnancy or Breastfeeding Dosage Information Drug Interactions Support Group En Español 39 Reviews Add your own review/rating Drug class: dopaminergic antiparkinsonism agents Consumer resources Rotigotine transdermal Rotigotine Rotigotine Transdermal (Advanced Reading) Professional resources Rotigotine (Wolters Kluwer) Other brands: Neupro Related treatment guides Parkinson's Disease Restless Legs Syndrome ]} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Drug Class Dopaminergic antiparkinsonism agents Related Drugs Restless Legs Syndrome ropinirole , pramipexole , Requip , Mirapex , levodopa , Horizant , gabapentin enacarbil , Neupro , More... Parkinson's Disease Exelon , ropinirole , pramipexole , Sinemet , Requip , benztropine , carbidopa / levodopa , Mirapex , amantadine , rivastigmine , Azilect , More... Rotigotine Rating 39 User Reviews 7.8 /10 39 User Reviews 7.8 Rate it!} } aggravating
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