Selegiline Transdermal System

Frampton, James E.; Plosker, Greg L.

doi:10.2165/00003495-200767020-00006

Cited by 28 publications

(6 citation statements)

References 16 publications

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“…The elimination half-life for the transdermal selegiline patch is 27.6 to 36.6 h [144,145]. For the pharmacokinetics of selegiline among the major depressive disorder population, the Cmax was 2.162 ng/mL after 18.4 h post application of the transdermal selegiline 6 mg/24 h patch [146]. The elimination half-life was 20.1 h [146].…”

Section: Transdermal Patches For Central Nervus System (Cns) Disordermentioning

confidence: 99%

Recent Advancement of Medical Patch for Transdermal Drug Delivery

et al. 2023

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Transdermal patches are a non-invasive method of drug administration. It is an adhesive patch designed to deliver a specific dose of medication through the skin and into the bloodstream throughout the body. Transdermal drug delivery has several advantages over other routes of administration, for instance, it is less invasive, patient-friendly, and has the ability to bypass first-pass metabolism and the destructive acidic environment of the stomach that occurs upon the oral ingestion of drugs. For decades, transdermal patches have attracted attention and were used to deliver drugs such as nicotine, fentanyl, nitroglycerin, and clonidine to treat various diseases or conditions. Recently, this method is also being explored as a means of delivering biologics in various applications. Here, we review the existing literatures on the design and usage of medical patches in transdermal drug delivery, with a focus on the recent advances in innovation and technology that led to the emergence of smart, dissolvable/biodegradable, and high-loading/release, as well as 3D-printed patches.

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Section: Transdermal Patches For Central Nervus System (Cns) Disordermentioning

confidence: 99%

Recent Advancement of Medical Patch for Transdermal Drug Delivery

et al. 2023

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“…This dosage and application overcomes the MAO-B selectivity and leads to MAO-A inhibition, seen to be necessary for antidepressive effects. In several controlled studies selegiline transdermal system exhibited significant treatment effects on MDD including core depression symptoms, vegetative symptoms and motor retardation (Frampton and Plosker, 2007; Robinson et al, 2007). A combination of selegiline and 5-hydroxytryptophan has been tested in a pilot study and proved antidepressant efficacy (Mendlewicz and Youdim, 1978).…”

Section: Indications In Parkinson's Diseasementioning

confidence: 99%

“…The bioavailability of selegiline when given as "melting-tablet" is more homogene and better reproduceable compared to the peroral type of application (Clarke et al, 2003a; 2003b). In addition a transdermal galenic form of selegiline has been developed for the treatment of major depression again reducing selegilines first-pass biotransformation (Frampton and Plosker, 2007; Robinson et al, 2007). …”

Section: Indications In Parkinson's Diseasementioning

confidence: 99%

MAO-inhibitors in Parkinson's Disease

Riederer¹,

2011

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Monoamine oxidase inhibitors (MAO-I) belong to the earliest drugs tried in Parkinson's disease (PD). They have been used with or without levodopa (L-DOPA). Non-selective MAO-I due to their side-effect/adverse reaction profile, like tranylcypromine have limited use in the treatment of depression in PD, while selective, reversible MAO-A inhibitors are recommended due to their easier clinical handling. For the treatment of akinesia and motor fluctuations selective irreversible MAO-B inhibitors selegiline and rasagiline are recommended. They are safe and well tolerated at the recommended daily doses. Their main differences are related to (1) metabolism, (2) interaction with CYP-enzymes and (3) quantitative properties at the molecular biological/genetic level. Rasagiline is more potent in clinical practise and has a hypothesis driven more favourable side effect/adverse reaction profile due to its metabolism to aminoindan. Both selegiline and rasagiline have a neuroprotective and neurorestaurative potential. A head-to head clinical trial would be of utmost interest from both the clinical outcome and a hypothesis-driven point of view. Selegiline is available as tablet and melting tablet for PD and as transdermal selegiline for depression, while rasagiline is marketed as tablet for PD. In general, the clinical use of MAO-I nowadays is underestimated. There should be more efforts to evaluate their clinical potency as antidepressants and antidementive drugs in addition to the final proof of their disease-modifying potential. In line with this are recent innovative developments of MAO-I plus inhibition of acetylcholine esterase for Alzheimer's disease as well as combined MAO-I and iron chelation for PD.

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“…TDDSs have the advantages of avoiding interference and degradation of the gastrointestinal tract and liver, improving the bioavailability and therapeutic effect of drugs, reducing side effects and discomfort, facilitating use in children and older adults, realizing local and systemic treatment, controlling the time of drug release, and having the ability to stop drug administration at any time [ 22 , 23 , 24 ]. The first transdermal patch for the treatment of depression was the Selegiline Transdermal System, which was marketed in 2006 [ 25 , 26 , 27 ]. Since the introduction of this patch, the development of transdermal antidepressant drug delivery systems has attracted considerable attention.…”

Section: Introductionmentioning

confidence: 99%

Establishment and Validation of a Transdermal Drug Delivery System for the Anti-Depressant Drug Citalopram Hydrobromide

Sun,

Ni,

Wang

et al. 2024

Molecules

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To enhance the bioavailability and antihypertensive effect of the anti-depressant drug citalopram hydrobromide (CTH) we developed a sustained-release transdermal delivery system containing CTH. A transdermal diffusion meter was first used to determine the optimal formulation of the CTH transdermal drug delivery system (TDDS). Then, based on the determined formulation, a sustained-release patch was prepared; its physical characteristics, including quality, stickiness, and appearance, were evaluated, and its pharmacokinetics and irritation to the skin were evaluated by applying it to rabbits and rats. The optimal formulation of the CTH TDDS was 49.2% hydroxypropyl methyl cellulose K100M, 32.8% polyvinylpyrrolidone K30, 16% oleic acid-azone, and 2% polyacrylic acid resin II. The system continuously released an effective dose of CTH for 24 h and significantly enhanced its bioavailability, with a higher area under the curve, good stability, and no skin irritation. The developed CTH TDDS possessed a sustained-release effect and good characteristics and pharmacokinetics; therefore, it has the potential for clinical application as an antidepressant.

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Selegiline Transdermal System

Cited by 28 publications

References 16 publications

Recent Advancement of Medical Patch for Transdermal Drug Delivery

Recent Advancement of Medical Patch for Transdermal Drug Delivery

MAO-inhibitors in Parkinson's Disease

Establishment and Validation of a Transdermal Drug Delivery System for the Anti-Depressant Drug Citalopram Hydrobromide

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