The efficiency of administering drugs trough transdermic systems

The efficiency of administering drugs trough transdermic systems

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Title: The efficiency of administering drugs trough transdermic systems
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Article_Title: The efficiency of administering drugs trough transdermic systems
Authors: Duka Robert, Melania Munteanu
Affiliation: “Vasile Goldiş” Western University Arad, Faculty of Medicine, Department of Pharmacy
“Vasile Goldiş” Western University Arad, Faculty of Medicine, Department of Pharmacy
Abstract: Transdermal delivery systems have become more increasingly important for treating neurologic and psychiatric disorders. Cholinesterase inhibitors have all been available in oral formulations but the rivastigmine patch was the first patch to be approved to treat Alzheimer’s disease (AD). The goal was to review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in Alzheimer’s disease. 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%). This treatment is well tolerated by patients because drug delivery is even and continuous, reducing fluctuation in drug plasma level, and attenuating the development of centrally mediated cholinergic side effects. Improved compliance with a subsequent drug administration may contribute to better clinical efficacy, reduce caregiver burden, result in a slower rate of institutionalization, and lead to a decrease in healthcare and medical costs. Because of these advantages, the rivastigmine patch has enabled great progress in treatment of AD, and may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.
Keywords: patch, transdermal delivery system, Alzheimer’s disease, rivastigmine, dementia
References: Sorin Leucuta, „Biofarmacie si Farmacocinetica”, Editura Dacia, Cluj Napoca 2002 pag 145-159
Rubin C.D. „The primary care of Alzheimer disease”. Am J Med Sci 2006 Dec; 332 (6): 314-33.
Fillit H., Cummings J. „Practice guidelines for the diagnosis and treatment of –Alzheimer’s disease in a managed care setting: part II. Pharmacologic therapy. -Alzheimer’s Disease Managed Care Advisory Council”. Manag Care Interface 2000 Jan; -13(1):51-6.
Lyketsos C.G., Colenda C.C., Beck C. et al. „Position statement of the American Association for Geriatric Psychiatry regarding principles of care patients with dementia resulting from Alzheimer disease”. Am J Geriatr Psychiatry 2006 Jul; 14 (7):561-73.
Lefevre G., Sedek G., Jhee S.S. et al. „Pharmacokinetics and pharmacodynamics of the novel daily rivastigmine transdermal patch compared with twice-daily capsules in Alzheimer’s disease patients”. Clin Pharmacol Ther. Epub 2007 May 23.
Priano L., Gasco M.R., Mauro „A. Transdermal treatment options for neurological disorders: impact on the elderly”. Drugs Aging 2006; 23 (5): 357-75.
Muhlack S., Przuntek H., Muller T. „Transdermal rivastigmine treatment does not worsen impaired performance of complex motion in patients with Alzheimer’s disease.” Pharmacopsychiatry 2006 Jan; 39 (1): 16-9.
Lefevre G., Sedek G., Huang H.L.A. et al. „Pharmacokinetics of a rivastigmine transdermal patch formulation in healthy volunteers: relative effects of bodz site application”. J Clin Pharmacol 2007 Apr; 47 (4): 471-8.
Lily Y., Gillian K. „Rivastigmine transdermal patch in the treatment of dementia of Alzheimer’s type”. CNS Drugs 2007; 21 (11): 957-965.
Winblad B., Cummings J., Andersen N. et al. „A six-month double –blind, randomized, placebo-controlled study of a transdermal patch in Alzheimer’s disease: rivastigmine patch versus capsule”. Int J Geriatr Psychiatry 2007 May; 22(5): 456-67.
Winbald B., Kawata A.K., Beusterien K.M. et al. „Caregiver preference for rivastigmine patch for rivastigmine patch relative to capsules for treatment of probable Alzheimer’s disease”. Int J Geriatr Psychiatry 2007 May: 22 (5): 485-91.
„American Psychiatric Association. Diagnostic and statistical manual of mental disorders”. 4th ed. Washington, Dc: American Psychiatric Association, 1994.
Berner B, John VA (February 1994). “Pharmacokinetic characterisation of transdermal delivery systems”. Clinical pharmacokinetics 26 (2): 121–34
Segal, Marian. “Patches, Pumps and Timed Release: New Ways to Deliver Drugs”. Food and Drug Administration. http://www.fda.gov/bbs/topics/consumer/CON00112.html.
Read_full_article: pdf/22-2012/22-4-2012/SU22-4-2012-Duka.pdf
Correspondence: Duka Robert, “Vasile Goldiş” Western University Arad, Faculty of Medicine, Department of Pharmacy, Romania, Tel: 0726 257108, email: rob_footprint@yahoo.com

Read full article
Article Title: The efficiency of administering drugs trough transdermic systems
Authors: Duka Robert, Melania Munteanu
Affiliation: “Vasile Goldiş” Western University Arad, Faculty of Medicine, Department of Pharmacy
“Vasile Goldiş” Western University Arad, Faculty of Medicine, Department of Pharmacy
Abstract: Transdermal delivery systems have become more increasingly important for treating neurologic and psychiatric disorders. Cholinesterase inhibitors have all been available in oral formulations but the rivastigmine patch was the first patch to be approved to treat Alzheimer’s disease (AD). The goal was to review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in Alzheimer’s disease. 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%). This treatment is well tolerated by patients because drug delivery is even and continuous, reducing fluctuation in drug plasma level, and attenuating the development of centrally mediated cholinergic side effects. Improved compliance with a subsequent drug administration may contribute to better clinical efficacy, reduce caregiver burden, result in a slower rate of institutionalization, and lead to a decrease in healthcare and medical costs. Because of these advantages, the rivastigmine patch has enabled great progress in treatment of AD, and may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.
Keywords: patch, transdermal delivery system, Alzheimer’s disease, rivastigmine, dementia
References: Sorin Leucuta, „Biofarmacie si Farmacocinetica”, Editura Dacia, Cluj Napoca 2002 pag 145-159
Rubin C.D. „The primary care of Alzheimer disease”. Am J Med Sci 2006 Dec; 332 (6): 314-33.
Fillit H., Cummings J. „Practice guidelines for the diagnosis and treatment of –Alzheimer’s disease in a managed care setting: part II. Pharmacologic therapy. -Alzheimer’s Disease Managed Care Advisory Council”. Manag Care Interface 2000 Jan; -13(1):51-6.
Lyketsos C.G., Colenda C.C., Beck C. et al. „Position statement of the American Association for Geriatric Psychiatry regarding principles of care patients with dementia resulting from Alzheimer disease”. Am J Geriatr Psychiatry 2006 Jul; 14 (7):561-73.
Lefevre G., Sedek G., Jhee S.S. et al. „Pharmacokinetics and pharmacodynamics of the novel daily rivastigmine transdermal patch compared with twice-daily capsules in Alzheimer’s disease patients”. Clin Pharmacol Ther. Epub 2007 May 23.
Priano L., Gasco M.R., Mauro „A. Transdermal treatment options for neurological disorders: impact on the elderly”. Drugs Aging 2006; 23 (5): 357-75.
Muhlack S., Przuntek H., Muller T. „Transdermal rivastigmine treatment does not worsen impaired performance of complex motion in patients with Alzheimer’s disease.” Pharmacopsychiatry 2006 Jan; 39 (1): 16-9.
Lefevre G., Sedek G., Huang H.L.A. et al. „Pharmacokinetics of a rivastigmine transdermal patch formulation in healthy volunteers: relative effects of bodz site application”. J Clin Pharmacol 2007 Apr; 47 (4): 471-8.
Lily Y., Gillian K. „Rivastigmine transdermal patch in the treatment of dementia of Alzheimer’s type”. CNS Drugs 2007; 21 (11): 957-965.
Winblad B., Cummings J., Andersen N. et al. „A six-month double –blind, randomized, placebo-controlled study of a transdermal patch in Alzheimer’s disease: rivastigmine patch versus capsule”. Int J Geriatr Psychiatry 2007 May; 22(5): 456-67.
Winbald B., Kawata A.K., Beusterien K.M. et al. „Caregiver preference for rivastigmine patch for rivastigmine patch relative to capsules for treatment of probable Alzheimer’s disease”. Int J Geriatr Psychiatry 2007 May: 22 (5): 485-91.
„American Psychiatric Association. Diagnostic and statistical manual of mental disorders”. 4th ed. Washington, Dc: American Psychiatric Association, 1994.
Berner B, John VA (February 1994). “Pharmacokinetic characterisation of transdermal delivery systems”. Clinical pharmacokinetics 26 (2): 121–34
Segal, Marian. “Patches, Pumps and Timed Release: New Ways to Deliver Drugs”. Food and Drug Administration. http://www.fda.gov/bbs/topics/consumer/CON00112.html.
*Correspondence: Duka Robert, “Vasile Goldiş” Western University Arad, Faculty of Medicine, Department of Pharmacy, Romania, Tel: 0726 257108, email: rob_footprint@yahoo.com