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Gillian M. Keating - One of the best experts on this subject based on the ideXlab platform.
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Rotigotine Transdermal Patch
CNS Drugs, 2008Co-Authors: Claudine M. Baldwin, Gillian M. KeatingAbstract:▴ Rotigotine is a non-ergolinic dopamine receptor agonist, formulated as a silicone-based Transdermal Patch, which has been evaluated for use in the treatment of adults with moderate to severe restless legs syndrome (RLS). ▴ Transdermal rotigotine improved the symptoms of RLS in two well designed 6-month trials in adults with idiopathic, moderate to severe RLS. Rotigotine (1–3 mg/24 h in one study and 2 or 3 mg/24 h in the other) decreased the International RLS Study Group Severity Rating Scale (IRLS) sum score and the Clinical Global Impression (CGI) item-1 assessment (severity of symptoms) from baseline (coprimary endpoints) to a significantly greater extent than placebo. Over half of rotigotine recipients were classified as treatment responders according to the IRLS sum score and CGI item-1 and item-2 ratings. ▴ Improvements in RLS symptoms have been maintained in the long term with rotigotine, according to the 3-year results of an open-label extension trial. ▴ Transdermal rotigotine was generally well tolerated in clinical trials and long-term extension studies in patients with moderate to severe RLS. ▴ There was a low risk of augmentation (i.e. intensification of RLS symptoms) with rotigotine, although further evaluations are required to ascertain if continuous dopaminergic stimulation has the effect of limiting or preventing augmentation.
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Rotigotine Transdermal Patch: in restless legs syndrome.
CNS drugs, 2008Co-Authors: Claudine M. Baldwin, Gillian M. KeatingAbstract:▴ Rotigotine is a non-ergolinic dopamine receptor agonist, formulated as a silicone-based Transdermal Patch, which has been evaluated for use in the treatment of adults with moderate to severe restless legs syndrome (RLS).
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Rotigotine Transdermal Patch
CNS Drugs, 2007Co-Authors: Claudine M. Baldwin, Gillian M. KeatingAbstract:A Transdermal Patch formulation of the non-ergolinic dopamine agonist rotigotine (Neupro®) is indicated for use as monotherapy in the treatment of early-stage Parkinson’s disease or, in the EU, as an adjunct to levodopa across all disease stages. Transdermal rotigotine is an effective and generally well tolerated addition to the armamentarium for the control of Parkinson’s disease, with the once-daily Transdermal Patch system offering several practical advantages and the possible benefits of avoiding pulsatile dopaminergic stimulation. Transdermal rotigotine was superior to placebo in patients with early-stage and advanced Parkinson’s disease, although noninferiority to the oral dopamine agonists ropinirole or pramipexole was not consistently demonstrated. Additional active comparator trials would be of interest. In the meantime, Transdermal rotigotine offers a convenient new treatment option for patients with Parkinson’s disease. Pharmacological Properties Rotigotine has agonist effects at all dopamine receptors in vitro , with the greatest affinity for, and activity at, the dopamine D_3 receptor subtype. It also interacts to some extent with α_2B- and α_2C-adrenergic receptors, serotonin 5-HT_1A and 5-HT_7 receptors, and σ receptors, and to a minor extent with monoamine transporters. The beneficial effects of rotigotine in the treatment of Parkinson’s disease are thought to be mediated via activation of D_1, D_2 and D_3 dopaminergic receptors within the caudate putamen. Rotigotine has demonstrated antiparkinsonian and potential neuroprotective effects in animal models of Parkinson’s disease. A stable drug-release profile is maintained over 24 hours, with steady-state plasma concentrations of rotigotine reached after approximately 2–3 days in healthy volunteers. The pharmacokinetic profile of Transdermal rotigotine does not differ according to Patch application site, although there is wide interindividual variability in rotigotine exposure after Patch application. Therapeutic Efficacy Transdermal rotigotine dose-dependently improved combined Unified Parkinson’s Disease Rating Scale (UPDRS) Activities of Daily Living (ADL) and motor subtotal scores in patients with early-stage Parkinson’s disease. The antiparkinsonian effects of Transdermal rotigotine were significant when compared with placebo, although noninferiority to oral ropinirole in terms of response rates (proportion of patients with a ≥20% decrease from baseline in combined UPDRS ADL and motor subtotal scores) was not shown. The proportion of treatment responders was significantly higher in Transdermal rotigotine than placebo recipients, as were Clinical Global Impression (CGI) scale scores. In longer-term trials, the benefits of Transdermal rotigotine were maintained for periods of at least 12 months. In patients with advanced Parkinson’s disease, Transdermal rotigotine as adjunctive therapy to levodopa significantly reduced ‘off’ time (periods during which symptoms are not masked by medication) and increased response rates (the percentage of patients achieving a ≥30% reduction in ‘off’ time); Transdermal rotigotine also had significant effects on the number of daily ‘off’ periods, ‘on’ time (periods when symptoms are well controlled) without troublesome dyskinesias, and combined UPDRS ADL and motor subtotal scores compared with placebo. Noninferiority of Transdermal rotigotine to oral pramipexole was shown with respect to changes in absolute ‘off’ time but not with respect to responder rates. Tolerability Transdermal rotigotine is generally well tolerated and has a tolerability profile considered typical of a dopamine receptor agonist, with the exception of application-site reactions such as erythema, pruritus and dermatitis. Adverse events occurring in significantly more Transdermal rotigotine than placebo recipients included nausea, vomiting, somnolence and fatigue. Across trials, other dopaminergic adverse events included hallucinations, peripheral oedema and orthostatic hypotension.
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Rivastigmine Transdermal Patch
CNS Drugs, 2007Co-Authors: Lily P. H. Yang, Gillian M. KeatingAbstract:▴ The cholinesterase inhibitor rivastigmine is now available as a Transdermal Patch for use in the treatment of mild to moderate dementia of the Alzheimer’s type. ▴ The Transdermal Patch gradually releases rivastigmine over the application period. There was less fluctuation between plasma peak and trough rivastigmine concentrations with the Patch than with the capsule formulation. ▴ The rivastigmine 9.5 mg/24 hours Patch was effective in patients with Alzheimer’s disease, according to the results of a well designed, 24-week trial. A significant improvement in Alzheimer’s Disease Assessment Scale —Cognitive subscale (ADAS-Cog) scores and significantly lower Alzheimer’s Disease Cooperative Study —Clinical Global Impression of Change scores were seen with the rivastigmine 9.5 mg/24 hours Patch versus placebo. ▴ In addition, treatment with the rivastigmine 9.5 mg/ 24 hours Patch was noninferior to rivastigmine 6mg twice-daily capsules, as assessed by ADAS-Cog scores. Significantly more caregivers of study patients preferred administering the Patch formulation of rivastigmine than the capsule formulation. ▴ The rivastigmine 9.5 mg/24 hours Patch was generally well tolerated by patients with Alzheimer’s disease. The incidence of adverse events (including nausea and vomiting) in the rivastigmine 9.5 mg/ 24 hours Patch group was not significantly different to that in the placebo group. However, several adverse events such as nausea and vomiting occurred in significantly more rivastigmine capsule recipients than in placebo recipients.
Anna Sauerbier - One of the best experts on this subject based on the ideXlab platform.
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rotigotine Transdermal Patch and sleep in parkinson s disease where are we now
npj Parkinson's disease, 2017Co-Authors: Mubasher A. Qamar, Raquel N. Taddei, Javier Pagonabarraga, Jaime Kulisevsky, Anna Sauerbier, Miguel RosagriloAbstract:A wide range of sleep dysfunction complicates Parkinson’s disease during its course from prodromal to palliative stage. It is now increasingly acknowledged that sleep disturbances are thus integral to the disease and pose a significant burden impacting on quality of life of patients. Sleep fragmentation, restless legs syndrome, nocturia, and nocturnal pain are regarded as one of the main components of night-time sleep dysfunction with possible secondary impact on cognition and well-being. The role of dopaminergic therapies, particularly using a continuous drug delivery strategy in managing some of these sleep issues, have been reported but the overall concept remains unclear. This review provides an overview of several aspects of night-time sleep dysfunction in Parkinson’s disease and describes all available published open-label and blinded studies that investigated the use of rotigotine Transdermal Patch targeting sleep. Blinded studies have suggested beneficial effects of rotigotine Transdermal Patch on maintenance insomnia and restless legs syndrome in Parkinson’s disease patients. Open-label studies support these observations and also suggest beneficial effects on nocturia and nocturnal pain.
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Rotigotine Transdermal Patch and sleep in Parkinson’s disease: where are we now?
Nature Publishing Group, 2017Co-Authors: Miguel Rosa-grilo, Mubasher A. Qamar, Raquel N. Taddei, Javier Pagonabarraga, Jaime Kulisevsky, Anna Sauerbier, Ray K. ChaudhuriAbstract:Abstract A wide range of sleep dysfunction complicates Parkinson’s disease during its course from prodromal to palliative stage. It is now increasingly acknowledged that sleep disturbances are thus integral to the disease and pose a significant burden impacting on quality of life of patients. Sleep fragmentation, restless legs syndrome, nocturia, and nocturnal pain are regarded as one of the main components of night-time sleep dysfunction with possible secondary impact on cognition and well-being. The role of dopaminergic therapies, particularly using a continuous drug delivery strategy in managing some of these sleep issues, have been reported but the overall concept remains unclear. This review provides an overview of several aspects of night-time sleep dysfunction in Parkinson’s disease and describes all available published open-label and blinded studies that investigated the use of rotigotine Transdermal Patch targeting sleep. Blinded studies have suggested beneficial effects of rotigotine Transdermal Patch on maintenance insomnia and restless legs syndrome in Parkinson’s disease patients. Open-label studies support these observations and also suggest beneficial effects on nocturia and nocturnal pain
Claudine M. Baldwin - One of the best experts on this subject based on the ideXlab platform.
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Rotigotine Transdermal Patch
CNS Drugs, 2008Co-Authors: Claudine M. Baldwin, Gillian M. KeatingAbstract:▴ Rotigotine is a non-ergolinic dopamine receptor agonist, formulated as a silicone-based Transdermal Patch, which has been evaluated for use in the treatment of adults with moderate to severe restless legs syndrome (RLS). ▴ Transdermal rotigotine improved the symptoms of RLS in two well designed 6-month trials in adults with idiopathic, moderate to severe RLS. Rotigotine (1–3 mg/24 h in one study and 2 or 3 mg/24 h in the other) decreased the International RLS Study Group Severity Rating Scale (IRLS) sum score and the Clinical Global Impression (CGI) item-1 assessment (severity of symptoms) from baseline (coprimary endpoints) to a significantly greater extent than placebo. Over half of rotigotine recipients were classified as treatment responders according to the IRLS sum score and CGI item-1 and item-2 ratings. ▴ Improvements in RLS symptoms have been maintained in the long term with rotigotine, according to the 3-year results of an open-label extension trial. ▴ Transdermal rotigotine was generally well tolerated in clinical trials and long-term extension studies in patients with moderate to severe RLS. ▴ There was a low risk of augmentation (i.e. intensification of RLS symptoms) with rotigotine, although further evaluations are required to ascertain if continuous dopaminergic stimulation has the effect of limiting or preventing augmentation.
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Rotigotine Transdermal Patch: in restless legs syndrome.
CNS drugs, 2008Co-Authors: Claudine M. Baldwin, Gillian M. KeatingAbstract:▴ Rotigotine is a non-ergolinic dopamine receptor agonist, formulated as a silicone-based Transdermal Patch, which has been evaluated for use in the treatment of adults with moderate to severe restless legs syndrome (RLS).
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Rotigotine Transdermal Patch
CNS Drugs, 2007Co-Authors: Claudine M. Baldwin, Gillian M. KeatingAbstract:A Transdermal Patch formulation of the non-ergolinic dopamine agonist rotigotine (Neupro®) is indicated for use as monotherapy in the treatment of early-stage Parkinson’s disease or, in the EU, as an adjunct to levodopa across all disease stages. Transdermal rotigotine is an effective and generally well tolerated addition to the armamentarium for the control of Parkinson’s disease, with the once-daily Transdermal Patch system offering several practical advantages and the possible benefits of avoiding pulsatile dopaminergic stimulation. Transdermal rotigotine was superior to placebo in patients with early-stage and advanced Parkinson’s disease, although noninferiority to the oral dopamine agonists ropinirole or pramipexole was not consistently demonstrated. Additional active comparator trials would be of interest. In the meantime, Transdermal rotigotine offers a convenient new treatment option for patients with Parkinson’s disease. Pharmacological Properties Rotigotine has agonist effects at all dopamine receptors in vitro , with the greatest affinity for, and activity at, the dopamine D_3 receptor subtype. It also interacts to some extent with α_2B- and α_2C-adrenergic receptors, serotonin 5-HT_1A and 5-HT_7 receptors, and σ receptors, and to a minor extent with monoamine transporters. The beneficial effects of rotigotine in the treatment of Parkinson’s disease are thought to be mediated via activation of D_1, D_2 and D_3 dopaminergic receptors within the caudate putamen. Rotigotine has demonstrated antiparkinsonian and potential neuroprotective effects in animal models of Parkinson’s disease. A stable drug-release profile is maintained over 24 hours, with steady-state plasma concentrations of rotigotine reached after approximately 2–3 days in healthy volunteers. The pharmacokinetic profile of Transdermal rotigotine does not differ according to Patch application site, although there is wide interindividual variability in rotigotine exposure after Patch application. Therapeutic Efficacy Transdermal rotigotine dose-dependently improved combined Unified Parkinson’s Disease Rating Scale (UPDRS) Activities of Daily Living (ADL) and motor subtotal scores in patients with early-stage Parkinson’s disease. The antiparkinsonian effects of Transdermal rotigotine were significant when compared with placebo, although noninferiority to oral ropinirole in terms of response rates (proportion of patients with a ≥20% decrease from baseline in combined UPDRS ADL and motor subtotal scores) was not shown. The proportion of treatment responders was significantly higher in Transdermal rotigotine than placebo recipients, as were Clinical Global Impression (CGI) scale scores. In longer-term trials, the benefits of Transdermal rotigotine were maintained for periods of at least 12 months. In patients with advanced Parkinson’s disease, Transdermal rotigotine as adjunctive therapy to levodopa significantly reduced ‘off’ time (periods during which symptoms are not masked by medication) and increased response rates (the percentage of patients achieving a ≥30% reduction in ‘off’ time); Transdermal rotigotine also had significant effects on the number of daily ‘off’ periods, ‘on’ time (periods when symptoms are well controlled) without troublesome dyskinesias, and combined UPDRS ADL and motor subtotal scores compared with placebo. Noninferiority of Transdermal rotigotine to oral pramipexole was shown with respect to changes in absolute ‘off’ time but not with respect to responder rates. Tolerability Transdermal rotigotine is generally well tolerated and has a tolerability profile considered typical of a dopamine receptor agonist, with the exception of application-site reactions such as erythema, pruritus and dermatitis. Adverse events occurring in significantly more Transdermal rotigotine than placebo recipients included nausea, vomiting, somnolence and fatigue. Across trials, other dopaminergic adverse events included hallucinations, peripheral oedema and orthostatic hypotension.
Vijay Veer - One of the best experts on this subject based on the ideXlab platform.
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Article Acute Dermal Irritation, Sensitization, and Acute Toxicity Studies of a Transdermal Patch for Prophylaxis Against (+)
2016Co-Authors: Subham Banerjee, Manash Pratim Pathak, Animesh Ghosh, Pronobesh Chattopadhyay, Shweta Singh, Vijay VeerAbstract:The skin irritating, sensitizing, and acute dermal toxicity potential of a novel combinational prophylactic Transdermal Patch, mainly composed of eserine and pralidoxime chloride as active pharmaceutical ingredients, against (+) anatoxin-a poisoning were investigated in rabbits, guinea pigs, and rats in compliance with the Organisation for Economic Cooperation and Development guidelines. In primary skin irritation test, rabbits were dermally attached with the therapeutically active Transdermal Patch or with a placebo Patch for 72 hours. The Transdermal Patches did not induce any adverse reactions such as erythema and edema on intact skin sites. The active Patch was classified as a practically nonirritating material based on the score in the primary irritation index. In the Buehler test, guinea pigs were sensitized by the active or placebo Transdermal Patches attached for 24 hours. The Patches did not induce any sensitization reactions in contrast to a severe sensitization reaction that occurred in the positive control. Therefore, the active Patch and placebo Patch were both graded as weak in sensitization score and rate. Acute dermal toxicity test in rats did not produce any overt signs of toxicity following a 14-day treatment period. Taken together, these findings suggest that the Transdermal Patch does not cause skin irritation, skin sensitization, or dermal toxic effects following dermal application
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protection by a Transdermal Patch containing eserine and pralidoxime chloride for prophylaxis against anatoxin a poisoning in rats
European Journal of Pharmaceutical Sciences, 2014Co-Authors: Subham Banerjee, Manash Pratim Pathak, Jyotchna Gogoi, Animesh Ghosh, Pronobesh Chattopadhyay, Vijay VeerAbstract:Abstract The prophylactic and neuroprotective impact of a Transdermal Patch containing eserine and pralidoxime chloride (2-PAM) against (±)-Anatoxin A poisoning was investigated using Wistar strain albino rats. Rats were smooth-shaved on the dorsal side, attached with a drug-in-adhesive matrix type prophylactic Transdermal Patch for 72 h and challenged with subcutaneous injection of three doses (1.0, 1.5 and 2.0 × LD 50 ) of (±)-Anatoxin A. The LD 50 value of (±)-Anatoxin A was determined to be 1.25 mg/kg, and at this particular dose (1.0 × LD 50 ) of toxin induced severe clinical symptom including extreme seizures in rats, resulting acute brain injuries in discrete brain regions, leading to 100% mortality within 5 min. The anticonvulsant effect, antiarrythmic effect, nerve conduction study, clinical observations and mortality, neuroprotective effect as well as skin histopathology of the prophylactic Transdermal Patch against (±)-Anatoxin A poisoning were investigated systematically. It was found that seizures, tachycardia, nerve damage, clinical symptoms, brain injuries and mortality induced by such lethal toxin were effectively prevented by the prophylactic Patch treatment up to certain LD 50 level. Hence, it could be a choice of potential therapeutic regimen against such lethal poisoning.
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accelerated stability testing of a Transdermal Patch composed of eserine and pralidoxime chloride for prophylaxis against anatoxin a poisoning
Journal of Food and Drug Analysis, 2014Co-Authors: Subham Banerjee, Shiv Sankar Bhattacharya, Amit Kundu, Animesh Ghosh, Pronobesh Chattopadhyay, Vijay VeerAbstract:The current study evaluated the stability potential of a Transdermal Patch composed of eserine and pralidoxime chloride for prophylaxis against (±)-anatoxin A poisoning. The drug combinations were fabricated in an adhesive matrix system supported by a backing membrane and attached to a temporary release liner. Stability testing of the optimized formulation was established for 6 months under accelerated study conditions as per International Conference on Harmonisation guidelines. Results obtained after 6 months showed that the optimized Patch formulation was stable with respect to drugs content, pH, diffusion, visual inspection, and other analytical parameters.
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Protection by a Transdermal Patch containing eserine and pralidoxime chloride for prophylaxis against (±)-Anatoxin A poisoning in rats.
European Journal of Pharmaceutical Sciences, 2014Co-Authors: Subham Banerjee, Manash Pratim Pathak, Jyotchna Gogoi, Animesh Ghosh, Pronobesh Chattopadhyay, Vijay VeerAbstract:Abstract The prophylactic and neuroprotective impact of a Transdermal Patch containing eserine and pralidoxime chloride (2-PAM) against (±)-Anatoxin A poisoning was investigated using Wistar strain albino rats. Rats were smooth-shaved on the dorsal side, attached with a drug-in-adhesive matrix type prophylactic Transdermal Patch for 72 h and challenged with subcutaneous injection of three doses (1.0, 1.5 and 2.0 × LD 50 ) of (±)-Anatoxin A. The LD 50 value of (±)-Anatoxin A was determined to be 1.25 mg/kg, and at this particular dose (1.0 × LD 50 ) of toxin induced severe clinical symptom including extreme seizures in rats, resulting acute brain injuries in discrete brain regions, leading to 100% mortality within 5 min. The anticonvulsant effect, antiarrythmic effect, nerve conduction study, clinical observations and mortality, neuroprotective effect as well as skin histopathology of the prophylactic Transdermal Patch against (±)-Anatoxin A poisoning were investigated systematically. It was found that seizures, tachycardia, nerve damage, clinical symptoms, brain injuries and mortality induced by such lethal toxin were effectively prevented by the prophylactic Patch treatment up to certain LD 50 level. Hence, it could be a choice of potential therapeutic regimen against such lethal poisoning.
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acute dermal irritation sensitization and acute toxicity studies of a Transdermal Patch for prophylaxis against anatoxin a poisoning
International Journal of Toxicology, 2013Co-Authors: Subham Banerjee, Manash Pratim Pathak, Animesh Ghosh, Pronobesh Chattopadhyay, Shweta Singh, Vijay VeerAbstract:The skin irritating, sensitizing, and acute dermal toxicity potential of a novel combinational prophylactic Transdermal Patch, mainly composed of eserine and pralidoxime chloride as active pharmaceutical ingredients, against (±) anatoxin-a poisoning were investigated in rabbits, guinea pigs, and rats in compliance with the Organisation for Economic Cooperation and Development guidelines. In primary skin irritation test, rabbits were dermally attached with the therapeutically active Transdermal Patch or with a placebo Patch for 72 hours. The Transdermal Patches did not induce any adverse reactions such as erythema and edema on intact skin sites. The active Patch was classified as a practically nonirritating material based on the score in the primary irritation index. In the Buehler test, guinea pigs were sensitized by the active or placebo Transdermal Patches attached for 24 hours. The Patches did not induce any sensitization reactions in contrast to a severe sensitization reaction that occurred in the pos...
Miguel Rosagrilo - One of the best experts on this subject based on the ideXlab platform.
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rotigotine Transdermal Patch and sleep in parkinson s disease where are we now
npj Parkinson's disease, 2017Co-Authors: Mubasher A. Qamar, Raquel N. Taddei, Javier Pagonabarraga, Jaime Kulisevsky, Anna Sauerbier, Miguel RosagriloAbstract:A wide range of sleep dysfunction complicates Parkinson’s disease during its course from prodromal to palliative stage. It is now increasingly acknowledged that sleep disturbances are thus integral to the disease and pose a significant burden impacting on quality of life of patients. Sleep fragmentation, restless legs syndrome, nocturia, and nocturnal pain are regarded as one of the main components of night-time sleep dysfunction with possible secondary impact on cognition and well-being. The role of dopaminergic therapies, particularly using a continuous drug delivery strategy in managing some of these sleep issues, have been reported but the overall concept remains unclear. This review provides an overview of several aspects of night-time sleep dysfunction in Parkinson’s disease and describes all available published open-label and blinded studies that investigated the use of rotigotine Transdermal Patch targeting sleep. Blinded studies have suggested beneficial effects of rotigotine Transdermal Patch on maintenance insomnia and restless legs syndrome in Parkinson’s disease patients. Open-label studies support these observations and also suggest beneficial effects on nocturia and nocturnal pain.