Levodopa ethylester: a novel rescue therapy for response fluctuations in Parkinson's disease

Annals of Neurology
R Djaldetti, E Melamed

Abstract

In Parkinson's disease (PD), response fluctuations may be due, in part, to pharmacokinetic problems including poor solubility of levodopa and difficulties in its absorption. We administered levodopa ethylester (LDEE), a new highly soluble prodrug of levodopa, by subcutaneous and intramuscular injections to PD patients with response fluctuations, in an open trial to examine its safety and efficacy. Various doses of LDEE (150-400 mg) turned patients "on" with a high success rate (43 of 45 injections). Latencies to "turning on" decreased and duration of on responses increased in a dose-dependent manner. LDEE, given either subcutaneously or intramuscularly, produced similar beneficial effects and induced rapid and sustained elevations in plasma levodopa levels. The drug was well tolerated with only minor and negligible side effects. Study suggests that subcutaneous and intramuscular administration of LDEE may be advantageous as a novel therapeutic strategy for response fluctuations. It may be particularly useful to rapidly and predictably res-cue patients from a variety of disabling "off" situations.

References

Jan 1, 1992·Movement Disorders : Official Journal of the Movement Disorder Society·F StocchiA Agnoli
Feb 1, 1990·Journal of Neurology, Neurosurgery, and Psychiatry·J P FrankelG M Stern
Jan 1, 1990·Movement Disorders : Official Journal of the Movement Disorder Society·J VaamondeJ A Obeso
Jan 1, 1989·Progress in Neuro-psychopharmacology & Biological Psychiatry·S RuggieriA Agnoli
Oct 1, 1974·British Journal of Clinical Pharmacology·S BergmannJ D Parkes

❮ Previous
Next ❯

Citations

Mar 29, 2002·Movement Disorders : Official Journal of the Movement Disorder Society·Ruth DjaldettiEldad Melamed
Apr 11, 2001·Movement Disorders : Official Journal of the Movement Disorder Society·A AlbaneseM Zappia
Oct 15, 1998·The New England Journal of Medicine·A E Lang, A M Lozano
Aug 5, 2003·Clinical Neuropharmacology·Doron MerimsEldad Melamed
Aug 9, 2006·Expert Review of Neurotherapeutics·Alan Diamond, Joseph Jankovic
Apr 23, 2009·Expert Opinion on Drug Delivery·Antonio Di StefanoLaura Serafina Cerasa
Feb 6, 2008·Expert Opinion on Drug Metabolism & Toxicology·Dag Nyholm, Hans Lennernäs
Jan 26, 2010·Expert Opinion on Drug Delivery·Ndidi NgwulukaDinesh Naidoo
Apr 13, 2012·Expert Opinion on Drug Discovery·Piera SozioAntonio Di Stefano
Oct 3, 2003·Expert Opinion on Pharmacotherapy·Janet RomrellMichael S Okun
Jan 4, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Fatma HaddadRafik Karaman
Jan 5, 2008·Movement Disorders : Official Journal of the Movement Disorder Society·Eldad MelamedRuth Djaldetti
Apr 21, 1999·European Journal of Neurology : the Official Journal of the European Federation of Neurological Societies·C Colosimo, M De Michele
Jul 1, 2016·Reviews in the Neurosciences·Joseph R PhillipsAhmed A Moustafa
Aug 8, 2021·Movement Disorders : Official Journal of the Movement Disorder Society·C Warren OlanowFabrizio Stocchi

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.