Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review
Summary Background: Cholinesterase inhibitors have all been available in oral formulations, but a rivastigmine transdermal patch has now been developed and is approved in many countries worldwide for the treatment of mild‐to‐moderate Alzheimer’s disease (AD) (including the USA, Latin America, Europ...
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| Veröffentlicht in: | International journal of clinical practice (Esher) 2009-05, Vol.63 (5), p.799-805 |
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| container_title | International journal of clinical practice (Esher) |
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| creator | Kurz, A. Farlow, M. Lefèvre, G. |
| description | Summary
Background: Cholinesterase inhibitors have all been available in oral formulations, but a rivastigmine transdermal patch has now been developed and is approved in many countries worldwide for the treatment of mild‐to‐moderate Alzheimer’s disease (AD) (including the USA, Latin America, Europe and Asia).
Objectives: To review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in dementia therapy. This article will also discuss how the patch may alter the treatment paradigm for patients with AD.
Results: The 9.5 mg/24 h rivastigmine patch was shown to provide comparable exposure to the highest recommended doses of capsules (12 mg/day) with significantly lower maximum plasma concentration (Cmax 8.7 vs. 21.6 ng/ml) and slower absorption rate (tmax 8.1 vs. 1.4 h). In a clinical trial of 1195 AD patients, this translated into similar efficacy with three times fewer reports of nausea and vomiting (7.2% vs. 23.1%, and 6.2% vs. 17.0% respectively). Consequently, more patients in the 9.5 mg/24 h patch group achieved their target therapeutic dose at the end of the study, compared with those in the 12 mg/day capsule group (95.9% vs. 64.4%).
Conclusion: The rivastigmine patch provides continuous drug delivery over 24 h and similar efficacy to the highest recommended dose of oral rivastigmine with improved tolerability. This may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment. |
| doi_str_mv | 10.1111/j.1742-1241.2009.02052.x |
| format | Article |
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Background: Cholinesterase inhibitors have all been available in oral formulations, but a rivastigmine transdermal patch has now been developed and is approved in many countries worldwide for the treatment of mild‐to‐moderate Alzheimer’s disease (AD) (including the USA, Latin America, Europe and Asia).
Objectives: To review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in dementia therapy. This article will also discuss how the patch may alter the treatment paradigm for patients with AD.
Results: The 9.5 mg/24 h rivastigmine patch was shown to provide comparable exposure to the highest recommended doses of capsules (12 mg/day) with significantly lower maximum plasma concentration (Cmax 8.7 vs. 21.6 ng/ml) and slower absorption rate (tmax 8.1 vs. 1.4 h). In a clinical trial of 1195 AD patients, this translated into similar efficacy with three times fewer reports of nausea and vomiting (7.2% vs. 23.1%, and 6.2% vs. 17.0% respectively). Consequently, more patients in the 9.5 mg/24 h patch group achieved their target therapeutic dose at the end of the study, compared with those in the 12 mg/day capsule group (95.9% vs. 64.4%).
Conclusion: The rivastigmine patch provides continuous drug delivery over 24 h and similar efficacy to the highest recommended dose of oral rivastigmine with improved tolerability. This may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.</description><identifier>ISSN: 1368-5031</identifier><identifier>EISSN: 1742-1241</identifier><identifier>DOI: 10.1111/j.1742-1241.2009.02052.x</identifier><identifier>PMID: 19392927</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Administration, Cutaneous ; Alzheimer Disease - drug therapy ; Alzheimer's disease ; Biological and medical sciences ; Biological Availability ; Cholinesterase Inhibitors - administration & dosage ; Cholinesterase Inhibitors - pharmacokinetics ; Degenerative and inherited degenerative diseases of the nervous system. Leukodystrophies. Prion diseases ; Drug Focus ; Drug therapy ; General aspects ; Humans ; Inhibitor drugs ; Medical sciences ; Neurology ; Pharmacology ; Phenylcarbamates - administration & dosage ; Phenylcarbamates - pharmacokinetics ; Prescription drugs ; Rivastigmine ; Transdermal medication ; Treatment Outcome</subject><ispartof>International journal of clinical practice (Esher), 2009-05, Vol.63 (5), p.799-805</ispartof><rights>2009 The Authors. Journal compilation © 2009 Blackwell Publishing Ltd</rights><rights>2009 INIST-CNRS</rights><rights>Journal compilation © 2009 Blackwell Publishing Ltd</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c6662-1a5bfde909e8950b8fa3738e8cfded12875e5602bbbd274133bcf112f3f422533</citedby><cites>FETCH-LOGICAL-c6662-1a5bfde909e8950b8fa3738e8cfded12875e5602bbbd274133bcf112f3f422533</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fj.1742-1241.2009.02052.x$$EPDF$$P50$$Gwiley$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fj.1742-1241.2009.02052.x$$EHTML$$P50$$Gwiley$$Hfree_for_read</linktohtml><link.rule.ids>230,314,780,784,885,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=21315920$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19392927$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kurz, A.</creatorcontrib><creatorcontrib>Farlow, M.</creatorcontrib><creatorcontrib>Lefèvre, G.</creatorcontrib><title>Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review</title><title>International journal of clinical practice (Esher)</title><addtitle>Int J Clin Pract</addtitle><description>Summary
Background: Cholinesterase inhibitors have all been available in oral formulations, but a rivastigmine transdermal patch has now been developed and is approved in many countries worldwide for the treatment of mild‐to‐moderate Alzheimer’s disease (AD) (including the USA, Latin America, Europe and Asia).
Objectives: To review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in dementia therapy. This article will also discuss how the patch may alter the treatment paradigm for patients with AD.
Results: The 9.5 mg/24 h rivastigmine patch was shown to provide comparable exposure to the highest recommended doses of capsules (12 mg/day) with significantly lower maximum plasma concentration (Cmax 8.7 vs. 21.6 ng/ml) and slower absorption rate (tmax 8.1 vs. 1.4 h). In a clinical trial of 1195 AD patients, this translated into similar efficacy with three times fewer reports of nausea and vomiting (7.2% vs. 23.1%, and 6.2% vs. 17.0% respectively). Consequently, more patients in the 9.5 mg/24 h patch group achieved their target therapeutic dose at the end of the study, compared with those in the 12 mg/day capsule group (95.9% vs. 64.4%).
Conclusion: The rivastigmine patch provides continuous drug delivery over 24 h and similar efficacy to the highest recommended dose of oral rivastigmine with improved tolerability. This may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.</description><subject>Administration, Cutaneous</subject><subject>Alzheimer Disease - drug therapy</subject><subject>Alzheimer's disease</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Cholinesterase Inhibitors - administration & dosage</subject><subject>Cholinesterase Inhibitors - pharmacokinetics</subject><subject>Degenerative and inherited degenerative diseases of the nervous system. Leukodystrophies. Prion diseases</subject><subject>Drug Focus</subject><subject>Drug therapy</subject><subject>General aspects</subject><subject>Humans</subject><subject>Inhibitor drugs</subject><subject>Medical sciences</subject><subject>Neurology</subject><subject>Pharmacology</subject><subject>Phenylcarbamates - administration & dosage</subject><subject>Phenylcarbamates - pharmacokinetics</subject><subject>Prescription drugs</subject><subject>Rivastigmine</subject><subject>Transdermal medication</subject><subject>Treatment Outcome</subject><issn>1368-5031</issn><issn>1742-1241</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>24P</sourceid><sourceid>WIN</sourceid><sourceid>EIF</sourceid><recordid>eNqNkU1v1DAQhi0EomXhL6AICTgl2OM4iTlUqlbQDyrYAwipF8txJo23-Vjs7HbLr8dhV1vghC-2PM-8emdeQiJGExbOu2XC8hRiBilLgFKZUKACku0jcnwoPA5vnhWxoJwdkWfeLykFIQr6lBwxySVIyI9Jt2i067QZbm2PozU-GupIR_2wwTYane59haHeRs5utB_tTRe4aKVH00T14KKxwYChHjvsx6n3tP3ZoO3QvfVRZT1qj--DoMONxbvn5EmtW48v9veMfPv44ev8PL76cnYxP72KTZZlwb4WZV2hpBILKWhZ1JrnvMDChN-KQZELFBmFsiwryFPGeWlqxqDmdQogOJ-Rk53ual12WJngzelWrZzttLtXg7bq70pvG3UzbBTkPJVBYUbe7AXc8GONflSd9QbbVvc4rL0K684hFzKAr_4Bl8Pa9WE4BSAly4BDgIodZNzgvcP64IRRNQWqlmrKTU25qSlQ9TtQtQ2tL_-c5KFxn2AAXu8B7Y1u6xCZsf7AAeNMSKAPK7mzLd7_twF1cTlfTM8gEO8ErB9xexDQ7lZlOc-F-v75TF1ez-H8E1uoa_4LpnTNHQ</recordid><startdate>200905</startdate><enddate>200905</enddate><creator>Kurz, A.</creator><creator>Farlow, M.</creator><creator>Lefèvre, G.</creator><general>Blackwell Publishing Ltd</general><general>Wiley-Blackwell</general><general>Hindawi Limited</general><scope>BSCLL</scope><scope>24P</scope><scope>WIN</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QP</scope><scope>7T5</scope><scope>7TK</scope><scope>7TS</scope><scope>7U9</scope><scope>H94</scope><scope>K9.</scope><scope>NAPCQ</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>5PM</scope></search><sort><creationdate>200905</creationdate><title>Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review</title><author>Kurz, A. ; Farlow, M. ; Lefèvre, G.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c6662-1a5bfde909e8950b8fa3738e8cfded12875e5602bbbd274133bcf112f3f422533</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Administration, Cutaneous</topic><topic>Alzheimer Disease - drug therapy</topic><topic>Alzheimer's disease</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Cholinesterase Inhibitors - administration & dosage</topic><topic>Cholinesterase Inhibitors - pharmacokinetics</topic><topic>Degenerative and inherited degenerative diseases of the nervous system. Leukodystrophies. Prion diseases</topic><topic>Drug Focus</topic><topic>Drug therapy</topic><topic>General aspects</topic><topic>Humans</topic><topic>Inhibitor drugs</topic><topic>Medical sciences</topic><topic>Neurology</topic><topic>Pharmacology</topic><topic>Phenylcarbamates - administration & dosage</topic><topic>Phenylcarbamates - pharmacokinetics</topic><topic>Prescription drugs</topic><topic>Rivastigmine</topic><topic>Transdermal medication</topic><topic>Treatment Outcome</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kurz, A.</creatorcontrib><creatorcontrib>Farlow, M.</creatorcontrib><creatorcontrib>Lefèvre, G.</creatorcontrib><collection>Istex</collection><collection>Wiley Online Library Open Access</collection><collection>Wiley Online Library Free Content</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Immunology Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Physical Education Index</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Premium</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>International journal of clinical practice (Esher)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kurz, A.</au><au>Farlow, M.</au><au>Lefèvre, G.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review</atitle><jtitle>International journal of clinical practice (Esher)</jtitle><addtitle>Int J Clin Pract</addtitle><date>2009-05</date><risdate>2009</risdate><volume>63</volume><issue>5</issue><spage>799</spage><epage>805</epage><pages>799-805</pages><issn>1368-5031</issn><eissn>1742-1241</eissn><abstract>Summary
Background: Cholinesterase inhibitors have all been available in oral formulations, but a rivastigmine transdermal patch has now been developed and is approved in many countries worldwide for the treatment of mild‐to‐moderate Alzheimer’s disease (AD) (including the USA, Latin America, Europe and Asia).
Objectives: To review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in dementia therapy. This article will also discuss how the patch may alter the treatment paradigm for patients with AD.
Results: The 9.5 mg/24 h rivastigmine patch was shown to provide comparable exposure to the highest recommended doses of capsules (12 mg/day) with significantly lower maximum plasma concentration (Cmax 8.7 vs. 21.6 ng/ml) and slower absorption rate (tmax 8.1 vs. 1.4 h). In a clinical trial of 1195 AD patients, this translated into similar efficacy with three times fewer reports of nausea and vomiting (7.2% vs. 23.1%, and 6.2% vs. 17.0% respectively). Consequently, more patients in the 9.5 mg/24 h patch group achieved their target therapeutic dose at the end of the study, compared with those in the 12 mg/day capsule group (95.9% vs. 64.4%).
Conclusion: The rivastigmine patch provides continuous drug delivery over 24 h and similar efficacy to the highest recommended dose of oral rivastigmine with improved tolerability. This may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>19392927</pmid><doi>10.1111/j.1742-1241.2009.02052.x</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Administration, Cutaneous Alzheimer Disease - drug therapy Alzheimer's disease Biological and medical sciences Biological Availability Cholinesterase Inhibitors - administration & dosage Cholinesterase Inhibitors - pharmacokinetics Degenerative and inherited degenerative diseases of the nervous system. Leukodystrophies. Prion diseases Drug Focus Drug therapy General aspects Humans Inhibitor drugs Medical sciences Neurology Pharmacology Phenylcarbamates - administration & dosage Phenylcarbamates - pharmacokinetics Prescription drugs Rivastigmine Transdermal medication Treatment Outcome |
| title | Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review |
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